TW200806642A - Indanyl-and tetrahydronaphthyl-amino-azoline-compounds for combating animal pests - Google Patents

Indanyl-and tetrahydronaphthyl-amino-azoline-compounds for combating animal pests Download PDF

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TW200806642A
TW200806642A TW095143449A TW95143449A TW200806642A TW 200806642 A TW200806642 A TW 200806642A TW 095143449 A TW095143449 A TW 095143449A TW 95143449 A TW95143449 A TW 95143449A TW 200806642 A TW200806642 A TW 200806642A
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Markus Kordes
Christopher Koradin
Deborah L Culbertson
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Basf Ag
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/18—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/50—Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/28—Nitrogen atoms not forming part of a nitro radical

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  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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Abstract

Indanyl- and Tetrahydronaphthyl-amino-azoline compounds for combating animal pests The present invention relates to lndanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.

Description

200806642 九、發明說明： 【發明所屬之技術領域】 本發明係關於適用於對抗動物害蟲之二氫茚基-或四氫 萘基-胺基-唑啉化合物。本發明亦係關於用於對抗動物害 蟲之方法且係關於用於對抗動物害蟲之農業組合物。 【先前技術】 動物害蟲且尤其為昆蟲、物蛛類及線蟲毀壞生長中及已 收穫之作物且侵襲木質住宅及商用建築，並引起食物供給 及財產之巨大經濟損失。雖然大量殺蟲劑為已知的，但是 由於目標害蟲形成對該等藥劑之抗性之能力，正需要用於 對昆蟲、蜘蛛類及線蟲之新穎藥劑。 類似於式I之彼等者之化合物已描述於DE-A1963 192中。 然而，描述於DE-A1963192中之該等化合物在其活性上 或就其活性範圍之廣度而言為有限的。 因此’本發明之一目標為提供化合物，其具有良好殺蟲 活性且展示抵抗大量不同動物害蟲，尤其抵抗難以控制之 昆蟲、蜘蛛類及線蟲之廣泛活性範圍。 【發明内容】 已發現該等目標可藉由式j之二氫茚基·或四氫萘基·胺 基-唑啉化合物來達成：200806642 IX. Description of the Invention: TECHNICAL FIELD OF THE INVENTION The present invention relates to dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compounds suitable for combating animal pests. The invention also relates to methods for combating animal pests and to agricultural compositions for combating animal pests. [Prior Art] Animal pests, and especially insects, spiders and nematodes, destroy growing and harvested crops and invade wooden and commercial buildings, and cause huge economic losses in food supply and property. Although a large number of insecticides are known, novel agents for insects, arachnids, and nematodes are being needed due to the ability of target pests to develop resistance to such agents. Compounds similar to those of formula I have been described in DE-A 1963 192. However, the compounds described in DE-A 1963 192 are limited in their activity or in terms of the breadth of their range of activity. Thus, one of the objects of the present invention is to provide compounds which have good insecticidal activity and which exhibit a wide range of activity against a large number of different animal pests, especially against insects, arachnids and nematodes which are difficult to control. SUMMARY OF THE INVENTION It has been discovered that such targets can be achieved by a dihydroindenyl or tetrahydronaphthylamino-oxazoline compound of formula j:

式I ; 115703.doc 200806642 該化合物亦可藉由町兩個異構式來表示Formula I; 115703.doc 200806642 The compound can also be represented by two isomers of the town

ηη

為1或2 ; 為1、2、3或4，其中當m為大於丄時，基團R2可具有 相同或不同含義；Is 1 or 2; is 1, 2, 3 or 4, wherein when m is greater than 丄, the groups R2 may have the same or different meanings;

X 為〇、s、nr3，其中 係選自氫、氰基、硝基、曱醯基、C( = 〇)R3C、 CVC6燒基、C2-C6婦基、C2_C6快基、環炫 基、Ci-C6：^氧基、c2_c^基胺基、二（CyCA 基）胺基、（Cl-C6烷氧基）亞甲基、^-匕烷基亞磺 醯基、匕心烷基硫基（Cl_C6_alkylsulfenyl)或cv C6烷基磺醯基 ，其中上述基 團之脂族基團 中之碳 原子可帶有1個、2個或3個彼此獨立地選自由以 下基團組成之群之基團的任一組合··鹵素、氰 基、硝基、羥基、巯基、胺基、羧基、Ci-C6烷 基Ci-C6烷氧基、烯基氧基、C2_C6炔基氧 基 、CiA i烷氧基及CVC6烷基硫基，或 C(0)NR3aR3b 、 3ap 3b # 甘 (S02)NR r 、苯基、苯基氧基或 节基，後3個所提及之基團之每一者可未經取代 115703.doc 200806642 或經1至5個彼此獨立地選自由以下基團組成之群 之基團取代：鹵素、CVC6烷基、CVC6鹵烷基、 Ci-C6烷基硫基、鹵烷基硫基、CrCs烷氧基 &c1-c6鹵烷氧基；且其中 R3a&R3b各自獨立地選自氫、Ci-C6烷基、CVC6 鹵烷基、C2-C6烯基或C2-C6炔基； R3e係選自氫、CVC6烷基、c2-c6烯基、c2-c6炔 基、c3-c8環烷基、CVC6烷基硫基、（^-(：6烷 氧基、（CVC6烷基）胺基、二（CVC6烷基）胺 基、苯基及可為含有1個、2個、3個或4個選 自0、S及N之雜原子之單環或雙環5至1〇員 雜芳環的雜芳基； R1係選自氫、氰基、硝基、甲醯基、c(=0)Rlc、CVC6 燒基、C2-C6烯基、C2-C6炔基、C3-C8環烧基、Cl-C6 烧氧基、（CrC6烷氧基）亞甲基、Cl-c6烷基亞磺醯 基、C^C6烧基硫基或c「C6烧基續醢基，其中上述基 團之脂族基團中之碳原子可帶有丨個、2個或3個彼此 獨立地選自由以下基團組成之群之基團的任一組合： 鹵素、氰基、硝基、羥基、巯基、胺基、羧基、el_ C6烷基、cvc6烷氧基、c2_c6烯基氧基、炔基氧 基、CVC6鹵燒氧基及Ci_C6烧基硫基，或 C(0)NRH (s〇2)NRlaRlb、苯基、苯基氧基或节 基後3個所提及之基團之每一者可未經取代或經1至 5個彼此獨立地選自由以下基團組成之群之基團取 115703.doc 200806642 代：鹵素、cvc6烷基、CrCs鹵烷基、Ci-Cs烷基硫 基、Ci-C6鹵烷基硫基、d_C6烷氧基及（^·ί：6鹵烷氧 基；且其中X is 〇, s, nr3, wherein it is selected from the group consisting of hydrogen, cyano, nitro, fluorenyl, C(= 〇)R3C, CVC6 alkyl, C2-C6, C2_C6 fast radical, cycloscyclyl, Ci -C6: oxy, c2_c^ylamino, bis(CyCA)-amino, (Cl-C6 alkoxy)methylene, ^-decylalkylsulfinyl, fluorenylalkylthio ( Cl_C6_alkylsulfenyl) or a cv C6 alkylsulfonyl group, wherein the carbon atom in the aliphatic group of the above group may have one, two or three groups independently selected from the group consisting of the following groups. Any combination of halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, Ci-C6 alkyl Ci-C6 alkoxy, alkenyloxy, C2_C6 alkynyloxy, CiA i alkoxy And CVC6 alkylthio, or C(0)NR3aR3b, 3ap 3b #甘(S02)NR r , phenyl, phenyloxy or a benzyl group, each of the latter three groups may be Substituted 115703.doc 200806642 or substituted with 1 to 5 groups independently selected from the group consisting of halogen, CVC6 alkyl, CVC6 haloalkyl, Ci-C6 alkylthio, haloalkyl Sulfur, CrCs alkoxy & c1-c6 haloalkoxy And wherein R3a&R3b are each independently selected from hydrogen, Ci-C6 alkyl, CVC6 haloalkyl, C2-C6 alkenyl or C2-C6 alkynyl; R3e is selected from hydrogen, CVC6 alkyl, c2-c6 olefin , c2-c6 alkynyl, c3-c8 cycloalkyl, CVC6 alkylthio, (^-(:6 alkoxy, (CVC6 alkyl)amine, bis(CVC6 alkyl)amine, phenyl And may be a heteroaryl group containing 1, 2, 3 or 4 monocyclic or bicyclic 5 to 1 member heteroaryl rings selected from the heteroatoms of 0, S and N; R1 is selected from the group consisting of hydrogen and cyanide Base, nitro, formazan, c(=0)Rlc, CVC6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, Cl-C6 alkoxy, (CrC6 alkoxy a methylene group, a Cl-c6 alkylsulfinyl group, a C^C6 alkylthio group or a c"C6 alkyl group, wherein the carbon atom of the aliphatic group of the above group may have a hydrazine , 2 or 3, any combination of groups independently selected from the group consisting of: halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, el_C6 alkyl, cvc6 alkane Oxyl, c2_c6 alkenyloxy, alkynyloxy, CVC6 halooxyl and Ci_C6 alkylthio, or C(0)NRH(s〇2)NRlaRlb Each of the three groups mentioned after the phenyl, phenyloxy or the benzyl group may be unsubstituted or taken from 1 to 5 groups independently selected from the group consisting of the following groups: 115703. Doc 200806642 Generation: halogen, cvc6 alkyl, CrCs haloalkyl, Ci-Cs alkylthio, Ci-C6 haloalkylthio, d_C6 alkoxy and (^·ί:6 haloalkoxy;

Rla& Rlb各自獨立地選自氫、C广C6烷基、CVC6鹵烷 基、c2-c6烯基或c2-C6炔基；Rla& Rlb are each independently selected from the group consisting of hydrogen, C-C6 alkyl, CVC6 haloalkyl, c2-c6 alkenyl or c2-C6 alkynyl;

Rlc係選自氫、CrCs烷基、C2-C6烯基、c2-C6炔基、 C3-C8環烷基、烷基硫基、cvc6烷氧基、 (CrC6烷基）胺基、二（Cl_C6烷基）胺基、苯基及可 為含有1個、2個、3個或4個選自〇、s及N之雜原 子之單環或雙環5至10員雜芳環的雜芳基； R2 係選自鹵素、OH、SH、NH2、S03H、COOH、氰 基、豐氮基、硝基、甲醯基、C〇NH2、CSNH2、 CH=N-OH、CHsN-CKCVCd 烷基、C(=〇)r2c、 C(=S)R 、CVC6烧基、C2-C6烯基、C2-C6快基、C3-C8 環烷基、（VC6烷氧基、（^-(^烷基胺基、二（(：1-(：6烷 基）胺基、（VC：8烧基硫基、C2_C6烯基、c2-C6烯基氧 基、C2-C6烯基胺基、c2-C6浠基硫基' c2-C6炔基、 C2-C6炔基氧基、c2-C6炔基胺基、C2-C6炔基硫基、 Ci-C6烧基石黃醯基、Ci-C：6烧基亞碉ί基（Ci —c6-alkylsulfoxyl)、c2_c6烯基磺醯基、c2_C6炔基磺醯 基、（eve：6烷氧基）羰基、（C2_C6烯基氧基）羰基、（cv C6炔基氧基）-羰基、（C「C6烷基）羰基氧基、（c2-c6烯 基-)羰基-氧基或（C^C：6炔基-)羰基氧基、（c2_c6烯基） 罗反基-胺基’其中上述基團之脂族基團中之碳原子可 115703.doc 200806642 帶有1個、2個或3個彼此獨立地選自由以下基團組成 之群之基團的任一組合：齒素、氰基、硝基、羥基、 巯基、胺基、羧基、（VC6烷基、Ci-C6烷氧基、C2-C6 烯基氧基、C2_C0炔基氧基、Cl-C6鹵烷氧基及(^_(：6烷 基硫基， C(〇)NR2aR2b、（S〇2)NR2aR2b，其中 R及R2b各自獨立地選自氫、〇h、NH2、Ci_C6烷基、 c「c6_烷基、κ6烯基或c2_C6炔基； R2c係選自氫、Cl-c6烷基、C2_C6烯基、c2_C6炔基、 CVC8環烷基、（:烷氧基、（Ci_c6烷基）胺基、 二（C丨-c0烷基）胺基、肼基、（C1-C6烷基）肼基、二 (CrC6烷基）肼基、苯基及可為含有i個、2個、3 個或4個選自0、S及N之雜原子之單環或雙環5至 10員雜芳環的雜芳基； 基團Y-Ar或基團Y_Cy，其中 為單鍵、氧、硫、氮、Ci-C6烷二基或(^_(：6 烷二基氧基； 為笨基、奈基或含有1個、2個、3個或4個選 自2個氧、2個硫及3個氮原子之雜原子作為 J哀成員之單環或雙環5至10員雜芳環，其中 ΑΓ未經取代或可帶有1至5個彼此獨立地選自 由以下基團組成之群之基團的任一組合：鹵 素、氰基、硝基、羥基、酼基、胺基、羧 基、C1-C6燒基、Ci-C6_烧基、烷氧 115703.doc -10· 200806642 基、C2-C6浠基氧基、C2-C6快基氧基、 鹵烷氧基及CrG烷基硫基； cy為c^c】2環烷基，其未經取代或經1至5個彼 此獨立地選自由以下基團組成之群之基團取 代··鹵素、氰基、硝基、羥基、巯基、胺 基、羧基、cvc6烧基、Ci-Cj烷基、CVC6 燒氧基、CVC6烯基氧基、C2_C6炔基氧基、Rlc is selected from the group consisting of hydrogen, CrCs alkyl, C2-C6 alkenyl, c2-C6 alkynyl, C3-C8 cycloalkyl, alkylthio, cvc6 alkoxy, (CrC6 alkyl) amine, di(Cl_C6 An alkyl)amino group, a phenyl group and a heteroaryl group which may be a monocyclic or bicyclic 5 to 10 membered heteroaryl ring containing 1, 2, 3 or 4 hetero atoms selected from the group consisting of hydrazine, s and N; R2 is selected from the group consisting of halogen, OH, SH, NH2, S03H, COOH, cyano, nitrogen-rich, nitro, formazan, C〇NH2, CSNH2, CH=N-OH, CHsN-CKCVCd alkyl, C ( =〇)r2c, C(=S)R, CVC6 alkyl, C2-C6 alkenyl, C2-C6 fast radical, C3-C8 cycloalkyl, (VC6 alkoxy, (^-(^ alkylamino) , bis((:1-(:6 alkyl)amino group, (VC: 8-alkylthio group, C2_C6 alkenyl group, c2-C6 alkenyloxy group, C2-C6 alkenylamino group, c2-C6 fluorenyl group) Thio-c2-C6 alkynyl, C2-C6 alkynyloxy, c2-C6 alkynylamino, C2-C6 alkynylthio, Ci-C6 alkyl ruthenium, Ci-C: 6 alkyl carbazide (Ci-c6-alkylsulfoxyl), c2_c6 alkenylsulfonyl, c2_C6 alkynylsulfonyl, (eve:6 alkoxy)carbonyl, (C2_C6 alkenyloxy)carbonyl, (cv C6 alkynyloxy) -carbonyl, (C "C6 a carbonyloxy group, a (c2-c6 alkenyl-)carbonyl-oxy group or a (C^C:6 alkynyl-)carbonyloxy group, a (c2_c6 alkenyl) rosinyl-amino group wherein the above groups are The carbon atom in the aliphatic group may be 115703.doc 200806642 with any combination of 1, 2 or 3 groups independently selected from the group consisting of dentate, cyano, nitro , hydroxy, decyl, amine, carboxyl, (VC6 alkyl, Ci-C6 alkoxy, C2-C6 alkenyloxy, C2_C0 alkynyloxy, Cl-C6 haloalkoxy and (^_(:6) Alkylthio, C(〇)NR2aR2b, (S〇2)NR2aR2b, wherein R and R2b are each independently selected from hydrogen, 〇h, NH2, Ci_C6 alkyl, c"c6-alkyl, κ6 alkenyl or c2_C6 Alkynyl; R2c is selected from the group consisting of hydrogen, Cl-c6 alkyl, C2_C6 alkenyl, c2_C6 alkynyl, CVC8 cycloalkyl, (: alkoxy, (Ci_c6 alkyl) amine, di(C丨-c0 alkyl) An amine group, a fluorenyl group, a (C1-C6 alkyl) fluorenyl group, a bis(CrC6 alkyl) fluorenyl group, a phenyl group and may be one, two, three or four selected from 0, S and N a heterocyclic ring of a heterocyclic ring having a monocyclic or bicyclic 5 to 10 membered heteroaryl ring; a group Y-Ar or a group Y_Cy, wherein Is a single bond, oxygen, sulfur, nitrogen, Ci-C6 alkanediyl or (^_(:6 alkylenedioxy); is a stupid group, a naphthyl group or contains 1, 2, 3 or 4 a hetero atom of 2 oxygen, 2 sulfur and 3 nitrogen atoms as a monocyclic or bicyclic 5 to 10 membered heteroaryl ring of a J. member, wherein ΑΓ is unsubstituted or may have 1 to 5 independently selected from Any combination of groups of the following groups: halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, C1-C6 alkyl, Ci-C6-alkyl, alkoxy 115703.doc -10· 200806642, C2-C6 mercaptooxy, C2-C6 fast oxy, haloalkoxy and CrG alkylthio; cy is c^c]2 cycloalkyl, unsubstituted or via 1 to 5 groups independently selected from the group consisting of halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, cvc6 alkyl, Ci-Cj alkyl, CVC6 Oxyl, CVC6 alkenyloxy, C2_C6 alkynyloxy,

Ci-C：6鹵烷氧基及烷基硫基； 且其中鍵結於苯環之相鄰碳原子之基團R2可連同 該等碳原子形成稠合苯環、稠合飽和或部分不飽 和5員、6員或7員碳環或含有1個、2個、3個或4 個選自2個氧、2個硫及3個氮原子之雜原子作為 環成員之稠合5員、6員或7員雜環，且其中該稠 合環未經取代或可帶有1個、2個、3個或4個彼此 獨立地選自由以下基團組成之群之基團：幽素、 氰基、硝基、羥基、巯基、胺基、羧基、d_C6 烷基、c「c6烷氧基、C2_C6烯基氧基、C2_C6炔基 氧基、Ci-C6鹵烷氧基及Cl-C6烷基硫基； 或其對映異構體及/或其農業上及/或獸醫學上可接受之 鹽； 其限制條件為式1化合物不為2-(4-硫基-第三丁基-1-二氫茚 基胺基噁唑啉。 乂因此，本發明係關於式I之二氫茚基，或四氫萘基_胺基_ 唑啉化合物，或其對應異構體且係關於其農業上或獸醫學 上可接雙之鹽。該等化合物具有高殺蟲活性且對抵抗廣泛 115703.doc 200806642 :圍之動物害蟲’尤其對抵抗昆蟲，蛛類及線蟲具有活 =亦係關於對抗動物害蟲，尤其為民蟲、㈣類及 =触之方法’纟包括將動物害蟲、其棲息地、滋生地、食 物供給，動物害蟲正生長或可生長於其中之植物、種子、 土壞、區域、材料或環境’或待保護免受動物害蟲，尤立 為昆蟲、料類或線蟲之侵襲或侵染之材料 '植物、種 子、土壞、表面或空間與殺蟲有效量之至少一種式〗之二 氫茚基"·或四氫萘基_胺基·唑啉化合物及/或其至少一 業上可接受之鹽接觸。 辰 此外，本發明提供保護作物免受動物害蟲，尤其為昆 =、蜘蛛類或線蟲之侵襲或侵染之方法，“括將;乍物： 殺蟲有效量之至少一籀式I之-寄甘 ,, — ^禋八1之一虱茚基-或四氫萘基-胺基- ϋ坐琳化合物及/或其至少一種鹽接觸。 此外，本發明係關於較佳呈可直接噴霧之溶液、乳液、 糊狀物、油分散液、粉末、用於散播之材料、微塵形式或 呈顆粒形式之農業組合物，其包括與一或多種農藝學上可 接文之惰性固體載劑或液體載劑及（若須要）至少一種界面 活性劑混合之如上文所定義之至少一種式ζ的二氫節基·或 四氣奈基-胺基-嗤琳化合物或其鹽。 在習知技術中，已描述用於藥理學用途之二氫茚基_或 四鼠奈基-胺基-σ坐琳。Ci-C: 6 haloalkoxy and alkylthio; and wherein the group R2 bonded to an adjacent carbon atom of the benzene ring may form a fused benzene ring, fused or partially unsaturated together with the carbon atoms 5-, 6-, or 7-membered carbon ring or a fused 5-member, 6 containing 1, 2, 3, or 4 heteroatoms selected from 2 oxygen, 2 sulfur, and 3 nitrogen atoms Or a 7-membered heterocyclic ring, and wherein the fused ring is unsubstituted or may carry 1, 2, 3 or 4 groups independently of each other selected from the group consisting of: nuclein, cyanide Base, nitro, hydroxy, decyl, amine, carboxyl, d_C6 alkyl, c "c6 alkoxy, C2_C6 alkenyloxy, C2_C6 alkynyloxy, Ci-C6 haloalkoxy and Cl-C6 alkyl a thio group; or an enantiomer thereof and/or an agriculturally and/or veterinarily acceptable salt thereof; the limitation is that the compound of formula 1 is not 2-(4-thio-tert-butyl-1 - Dihydrofurfurylamine oxazoline. Accordingly, the present invention relates to a dihydroindenyl group of formula I, or a tetrahydronaphthyl-amino oxazoline compound, or a corresponding isomer thereof, and related to its agriculture Upper or veterinary science can be used to double salt. The substance has high insecticidal activity and is resistant to a wide range of 115703.doc 200806642: surrounding animal pests' especially against insects, spiders and nematodes live = also related to animal pests, especially for insects, (four) and = touch '纟 includes animal pests, their habitat, breeding grounds, food supplies, plants, seeds, soil, areas, materials or environments in which animal pests are growing or can be grown' or protected from animal pests, A material that is infested or infested by insects, mites or nematodes 'plant, seed, soil, surface or space and insecticidal effective amount of at least one formula of dihydroindolyl" or tetrahydronaphthyl-amine The oxazoline compound and/or at least one of the commercially acceptable salts thereof are contacted. In addition, the present invention provides a method for protecting crops from animal pests, particularly invasive or infested by Kunming, spiders or nematodes,乍 将; 乍 : : 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 乍 , , , , , , , , , , , At least one salt is contacted. Further, the invention is related to Preferred are sprayable solutions, emulsions, pastes, oil dispersions, powders, materials for spreading, dusty forms or agricultural compositions in the form of granules, including one or more agronomically achievable texts An inert solid carrier or liquid carrier and, if desired, at least one surfactant-mixed at least one dihydrogenated sulphate or tetras-n-yl-amino-anthracene compound as defined above or Salts In the prior art, dihydroindenyl or tetramethylnaphthyl-amino- sigma has been described for pharmacological use.

Wong，W.C·等人揭示2-胺基-2-噁唑琳之方便合成法及其 在選殖人類α-腎上腺素受體上之藥理學評估（Bi〇〇rg. &Wong, W.C. et al. disclose a convenient synthesis of 2-amino-2-oxazole and its pharmacological evaluation on the selection of human alpha-adrenergic receptors (Bi〇〇rg. &

Med. Chem· Lett，4(19)，1994，第 1217-22 頁）。 115703.doc -12· 200806642 氧曱α坐琳化合物之水解降解由Yamana，Τ·等人 (Yakuzaiguku (1967)，27(3)，第 203_5 頁）論述。 在ϋS 3,296,077 中，2-(l-四氫萘基胺基）-咪唑啉化合物 之存在可見於修整組合物中。亦在Nippon YakurigakuMed. Chem. Lett, 4 (19), 1994, pp. 1217-22). 115703.doc -12· 200806642 Hydrolysis degradation of oxonium-based compound is discussed by Yamana, Τ· et al. (Yakuzaiguku (1967), 27(3), p. 203_5). In ϋS 3,296,077, the presence of a 2-(l-tetrahydronaphthylamino)-imidazoline compound can be found in the conditioning composition. Also in Nippon Yakurigaku

Zasshi (1965)，61(6)，第479-89頁中描述2-(1-四氫萘基胺 基）-味嗤啉化合物之擬交感神經效應，在US 4,520,014中 描述其血管收縮效應或在Arzneimittelforschung 1962，12， 弟975-8頁中描述其於鼻用組合物中之功效。 US 2,883,410、US 2,870，161 及 US 2,870，159 描述 2-(1-二 氫茚基胺基）-噁唑啉作為醫藥組合物中之寧神劑，其中前 兩項專利揭示2-(4-硫基-第三丁基-丨_二氫茚基胺基>噁唑 琳。US 2,956,072揭示用於相同目的之2_(1_四氫萘基胺 基）-噁唑琳。 具有噻唑啉、噁唑啉或咪唑啉取代之2·(1_四氫萘基胺 基）-竹生物或2-(1- 一 IL茚基胺基）-衍生物可見於us 3,636,219及118 3,679,798中，其中描述其抗膽驗能效應。 芳基·胺基-噁唑啉或芳基-胺基-噻唑啉已在〇£_人丨963 192中作為殺蟲劑而討論或在DE_b 1 954 584中用於作物保 護而討論。 後兩個文獻皆未揭示衍生物，其揭示具有可比取代流程 之二氫茚基-或四氫萘基-胺基-唑啉，其中二氫茚基或四氫 萘基環系統之芳族部分係經取代。較佳地，二氣節某或 四氫萘基-胺基-唑啉係在位置A及/或C及/或〇處經取代。 較佳地，二氫茚基或四氫萘基環系統之非稠合部分保留未 115703.doc 13 200806642 取代狀態以及唑啉環系統保留未取代狀態。 式I化合物可具有一或多個對掌性中心，在該狀況下， 其以諸如對映異構體或非對映體之立體異構體之混合物存 在。本發明提供例如純對映異構體或純非對映體之純立體 異構體及其混合物。式1化合物亦可以不同互變異構體之 形式存在。本發明包括單一互變異構體，（若可分離)以及 互變異構體混合物。 根據本發明，適於使用之式1化合物之鹽尤其為農業上 可接又之鹽。其可以習用方法形成，例如若式“匕合物具 有驗生“b基，則藉由使化合物與所述陰離子之酸反應來 形成或藉由使式1之酸性化合物與適合鹼反應來形成。 適合之農業±適用帛尤其為彼等陽離子《鹽或彼等酸之 •夂力成1 .亥等鹽之陽離子及_離子分別冑根據本發明之 化合物之作用不具有任何不利影響。適合之陽離子尤其為 鹼金屬離子’較佳為鐘、納及鉀離子；驗土金屬離子，較 佳為轉、鎭及鋇離子；及過渡金屬離子，較佳為鑑、銅、 、年及鐵離子，亦及叙離子（NH4+)及經取代之銨離子，其中 氫原子之1至4者藉由Cl-C4烷基、Ci_c4羥基烷基、。{々烷 乳基、eve：4烷氧基-Cl-C4烷基、羥基_Ci_C4烷氧基_Ci_山 烷基、苯基及/或苄基置換。經取代之銨離子之實例包括 甲基鉍離子、異丙基銨離子、二甲基銨離子、二異丙基銨 離子、一甲基鏔離子、四甲基銨離子、四乙基銨離子、四 T基銨離子、2-羥基乙基銨離子、2_(2_羥基乙氧基）乙基 鉍離子、雙（2-羥基乙基）銨離子、苄基三甲基銨離子及苄 115703.doc -14 - 200806642 基三乙基銨離子，此外包括鱗離子、銃離子，較佳為三 (c〗-C4烷基）銃離子及氧化銕離子，較佳為三（Ci_C4烷基）氧 化疏離子。 適用酸加成鹽之陰離子主要為氣離子、溴離子、氟離 子、硫酸氫根、硫酸根、磷酸二氫根、磷酸氫根、碟酸 根、硝酸根、碳酸氫根、碳酸根、六氟矽酸根、六氟磷酸 根、苯甲酸根及C^C：4烷酸之陰離子，較佳為曱酸根、乙 酸根、丙酸根及丁酸根。其可藉由使式^匕合物與相應陰 離子之酸’較佳為鹽酸、氫溴酸、硫酸、磷酸或硝酸反應 來形成。 與術語鹵素類似，在上文變數之定義中所提及之有機部 分為個別基團成員之個別列表之集體術語。在各狀況下， 字首cn-cm指示基團中之碳原子之可能數目。 在各狀況中’術語鹵素表示氟、溴、氣或碘，尤其為 氟、氣或漠。 其他含義之實例為： 如本文中所使用及在(^-(^烷氧基、^-〇6烷基胺基、二 (CVC6烧基）胺基、CVC6烷基硫基、CVC6烷基磺醯基、CV C6烧基亞礙基、Cl_c6烷基羰基、Cl_c6烷氧基羰基、Cl-C6 烧基硫基Μ基及CrC6烷基羰基氧基之烷基部分中之術語 "C「C6烧基”係指具有1至6個碳原子之飽和直鏈或支鏈烴 基’尤其為1至4個碳之基團，例如甲基、乙基、丙基' κ 甲基乙基、丁基、1-甲基丙基、入甲基丙基、二甲基 乙基、戊基、1-甲基丁基、2_甲基丁基、3_甲基丁基、2,2、 115703.doc •15· 200806642 二曱基丙基、1-乙基丙基、己基、1，1-二甲基丙基、1，2-二 曱基丙基、1-甲基戊基、2-甲基戊基、3 -甲基戊基、4 -甲 基戊基、1，1-二甲基丁基、1，2-二曱基丁基、1，3·二甲基丁 基、2,2-二甲基丁基、2,3-二甲基丁基、3,3·二曱基丁基、 1_乙基丁基、2-乙基丁基、1，1，2·三甲基丙基、ΐ，2,2·三甲 基丙基、1-乙基-1-甲基丙基、1-乙基-2-甲基丙基、庚基、 辛基、2-乙基己基、壬基及癸基及其異構體。Cl-C4烷基意 謂（例如）甲基、乙基、丙基、1-甲基乙基、丁基、1-甲基 丙基、2 -甲基丙基或1，1-二甲基乙基。 如本文中所使用之術語"CrC6鹵烷基”係指具有個碳 原子之直鍵或支鍵飽和烧基（如上文所提及），其中該等基 團中之一些或所有氫原子可藉由如上文所提及之函素原子 置換，例如CrC4鹵烷基，諸如氯曱基、溴甲基、二氣甲 基、三氯甲基、氟甲基、二氟甲基、三氟曱基、氣氟曱 基、二氣氟甲基、氯二氟甲基、1·氯乙基、；[•漠乙基、 氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氣-2·氟乙基、2-氯-2,2_二氟乙基、2,2-二氯_2·氟乙基、2,2,2-三氯乙基、五氟乙基及其類似基團。 如本文中所使用之術語”C〗-C6烷氧基”係指經由氧原子連 接之具有1至6個碳原子之直鏈或支鏈飽和烷基（如上文所 提及）。實例包含Ci-C6烧氧基，諸如甲氧基、乙氧基、 OCH2-C2H5、〇CH(CH3)2、正 丁氧基 ' 〇CH(CH3)-C2H5、 OCH2-CH(CH3)2、oc(ch3)3、正戊氧基、卜甲基丁氧基、 2-甲基丁氧基、3-甲基丁氧基、i，卜二甲基丙氧基、i，孓二 115703.doc -16· 200806642 甲基丙氣基、2，2 -二甲基-丙氧基、卜乙基丙氧基、正己氧 基、1-甲基戊氧基、2-甲基戊氧基、3-甲基戊氧基、4-甲 基戊氧基、1，1-二甲基丁氧基、！，>二甲基丁氧基、！，弘二 曱基丁氧基、2,2-二甲基丁氧基、2,3-二曱基丁氧基、3,3-二曱基丁氧基、1-乙基丁氧基、2_乙基丁氧基、三甲 基丙氧基、1，2,2-三甲基丙氧基、卜乙基-1-曱基丙氧基、 1-乙基-2-f基丙氧基及其類似基團。 如本文中所使用之術語”CrQ鹵烷氧基”係指如上文所提 及之CrC6烷氧基，其中氫原子部分或全部經氟、氯、溴 及/或碘取代，亦即，例如Cl_C6鹵烷氧基，諸如氯曱氧 基、二氯甲氧基、三氯甲氧基、氟曱氧基、二氟甲氧基、 三氟甲氧基、氣氟甲氧基、二氣氟甲氧基、氯二氟曱氧 基、2·氟乙氧基、2-氣乙氧基、2-溴乙氧基、2-埃乙氧 基、2,2-二氟乙氧基、2,2,2-三氟乙氧基、2-氯-2-氟乙氧 基、2-氣-2,2_二氟乙氧基、2,2-二氯·2-氟乙氧基、2,2,2-三 氯乙氧基、五氟乙氧基、2-氟丙氧基、3_氟丙氧基、2,2 二氟丙氧基、2,3-二氟丙氧基、2_氯丙氧基、％氯丙氧 基、2,3-二氣丙氧基、2-溴丙氧基、3_溴丙氧基、3,3,3_三 氟丙氧基、3,3,3-三氯丙氧基、2,2,3,3,3_五氟丙氧基、六 氟丙氧基、1·(氟甲基)-2-氟乙氧基、！_(氣甲基)_2·氯乙氧 基、W漠甲基）-2-漠乙氧基、4_氟丁氧基、心氣丁氧基、 4-溴丁氧基、九氟丁氧基、5_氟-丨_戊氧基 5_氣-1-戊氧 ，基、 基、 5 -漠-1-戊氧基 十一氟戊氧基 -峨-1-戊氧基、5,5,5_三氣•戊氧 6-氯-1-己氧基、6_ 115703.doc -17- 200806642 1^己氧基、6-硤]-己氧基、6，m_三氯小己氧基或十二 氟己氧基，尤其為氯甲氧基、氟甲氧基、2氣甲氧基、三 氟甲氧基、2-氟乙氧基、2·氯乙氧基或2,2,2_三氟乙氧基。 如本文中所使用之術語”Cl_C6烷氧基^烷基"係指 烷基，其中丨個碳原子帶有丨個如上文所提及之 烷氧基。實例為CH^OCH3、CH2-OC2H5、正丙氧基甲基、 CH2-OCH(CH3)2、正丁氧基甲基、（1-甲基丙氧基）甲基、 (21基丙氧基）甲基、CH2_0C(CH3)3、2_(甲氧基）乙基、 (乙氧基)乙基、2-(正丙氧基)乙基、2 —(卜甲基乙氧基)乙 基、2-(正丁氧基）乙基、2_(1_甲基丙氧基）乙基、2分甲基 丙氧基）乙基、2-(1，1·二甲基乙氧基）乙基、2_(甲氧基）丙 基、2-(乙氧基）丙基、2_(正丙氧基）丙基、2_(卜甲基乙氧 基）丙基、2-(正丁氧基）丙基、2_〇_甲基丙氧基）丙基、2一 (2-甲基丙氧基）丙基、2_(u二甲基乙氧基）丙基、％(甲氧 基）丙基、3-(乙氧基）丙基、3-(正丙氧基）丙基、3_(1_甲基 乙氧基）丙基、3-(正丁氧基）丙基、3-(1-甲基丙氧基）丙 基、3-(2-甲基丙氧基）丙基、^，卜二甲基乙氧基）丙基、 2-(甲氧基）丁基、2_(乙氧基）丁基、2_(正丙氧基）丁基、2· (1-甲基乙氧基）丁基、2_(正丁氧基）丁基、2_(1_甲基丙氧 基）丁基、2-(2-甲基丙氧基）丁基、2_(1，卜二甲基乙氧基）丁 基、3_(甲氧基）丁基、3-(乙氧基）丁基、3_(正丙氧基）丁 基3(1-甲基乙氧基）丁基、3-(正丁氧基）丁基、•甲基 丙氧基）丁基、甲基丙氧基）丁基、3-(1，1-二甲基乙氧 基）丁基、4-(甲氧基）丁基、4_(乙氧基）丁基、4•(正丙氧基） 115703.doc •18- 200806642 丁基、4-(1-甲基乙氧基）丁基、4-(正丁氧基）丁基、4 _(卜甲 基丙氧基）丁基、4-(2-甲基丙氧基）丁基、‘（ij•二曱基乙 氧基）丁基及其類似基團。 如本文中所使用之術語”（Cl-C0烷基）羰基”係指經由羰基 之石反原子鍵結於烧基中之任一鍵處之具有1至6個碳原子的 直鏈或支鏈飽和烷基（如上文所提及）。實例包含Ci_C6烷基 羰基，諸如CO-CH3、CO-C2H5、正丙基羰基、丨-甲基乙基 罗厌基、正丁基幾基、1-甲基丙基魏基、2_甲基丙基幾基、 二曱基乙基羰基、正戊基羰基、1-曱基丁基羰基、2_ 甲基丁基羰基、3 -甲基丁基羰基、1，1_二甲基丙基羰基、 1，2_二甲基丙基羰基、2,2-二曱基丙基羰基、1-乙基丙基羰 基、正己基羰基、1-甲基戊基羰基、2-甲基戊基羰基、3_ 甲基戊基羰基、4-甲基戊基羰基、1，1_二甲基丁基羰基、 1，2-二曱基丁基羰基、I%二甲基丁基羰基、2,2_二甲基丁 基羰基、2,3-二甲基丁基羰基、3,3-二甲基丁基羰基、1·乙 基丁基羰基、2-乙基丁基羰基、l，i，2-三甲基丙基羰基、 1’2,2 -二甲基丙基幾基、1-乙基-1-甲基丙基幾基或ι_乙基_ 2-甲基丙基羰基及其類似基團。 如本文中所使用之術語"（CVC6烷氧基）羰基”係指經由羰 基之碳原子連接之具有1至6個碳原子的直鏈或支鏈烷氧基 (如上文所提及），例如 co-och3、CO-OC2H5、coo-ch2-C2H5、CO-OCH(CH3)2、正 丁氧基幾基、CO-OCHCCl·^)-c2H5、c〇-och2-ch(ch3)2、CO-OC(CH3)3、正戊氧基羰 基、1-甲基丁氧基羰基、2-甲基丁氧基羰基、3-甲基丁氧 115703.doc -19- 200806642 基技基、2,2-二甲基丙氧基羰基、卜乙基丙氧基羰基、正 己氧基羰基、二甲基丙氧基羰基、U2_二甲基丙氧基 罗厌基、1-甲基戊氧基羰基、2_甲基戊氧基羰基、3_甲基戊 氧基羰基、4-甲基戊氧基羰基、丨，卜二甲基丁氧基羰基、 1,2-二甲基丁氧基羰基、13-二甲基丁氧基羰基、2,2_二甲 基丁氧基羰基、2,3-二甲基丁氧基羰基、3,3_二甲基丁氧 基羰基、1-乙基丁氧基羰基、乙基丁氧基羰基、丨，12-三 甲基丙氧基羰基、；1，2,2_三甲基丙氧基羰基、丨_乙基·丨_甲 基丙氧基羰基或1-乙基-2-甲基丙氧基羰基。 如本文中所使用之術語”（Cl-C6烷基）羰基氧基"係指經由 羰基氧基之碳原子鍵結於烷基中之任一鍵處的具有丨至6個 碳原子之直鏈或支鏈飽和烷基（如上文所提及），例如〇_ CO-CH3、〇弋0-(：出5、正丙基羰基氧基、卜甲基乙基羰基 氧基、正丁基羰基氧基、丨_甲基丙基羰基氧基、2_曱基丙 基幾基氧基、1，1·二甲基乙基羰基氧基、正戊基羰基氧 基、1-甲基丁基羰基氧基、2-甲基丁基羰基氧基、弘甲基 丁基幾基氧基、1，1·二甲基丙基羰基氧基或1>2_二甲基丙 基羰基氧基。 如本文中所使用之術語”〇1-(：6烷基硫基（Cl-c6烷基硫 基：CrC6烷基-S-)"係指經由硫原子連接之具有1至6個碳 原子的直鏈或支鏈飽和烷基（如上文所提及），例如 基硫基，諸如甲基硫基、乙基硫基、丙基硫基、曱基乙 基硫基、丁基硫基、1-甲基丙基硫基、2_甲基丙基硫基、 1，1·二甲基乙基硫基、正戊基硫基、1-甲基丁基硫基、2_ 115703.doc -20- 200806642 曱基丁基硫基、3-甲基丁基硫基、2,2-二曱基丙基硫基、 1-乙基丙基硫基、正己基硫基、1，1_二甲基丙基硫基、丨，2_ 二曱基丙基硫基、1-甲基戊基硫基、2-曱基戊基硫基、3-甲基戊基硫基、4-甲基戊基硫基、ι，ι·二甲基丁基硫基、 1，2-二甲基丁基硫基、：ι，3-二甲基丁基硫基、2,2_二甲基丁 基硫基、2,3-二甲基丁基硫基、3,3-二甲基丁基硫基、1-乙 基丁基硫基、2-乙基丁基硫基、l，i，2-三甲基丙基硫基、 1，2,2 -二曱基丙基硫基、1-乙基-1-甲基丙基硫基或1 _乙基_ 2 -甲基丙基硫基。 如本文中所使用之術語，•（CrG烷基硫基）羰基"係指經由 羰基之碳原子連接之具有1至6個碳原子的直鏈或支鏈烷基 硫基（如上文所提及）。實例包含CO-SCH3、CO-SC2H5、 CO_SCH2-C2H5、CO-SCH(CH3)2、正丁 基硫基羰基、co-SCH(CH3)-C2H5、CO-SCH2-CH(CH3)2、CO-SC(CH3)3、正 戊基硫基羰基、1-甲基丁基硫基羰基、2-甲基丁基硫基羰 基、3-甲基丁基硫基羰基、2,2-二甲基丙基硫基羰基、1-乙基丙基硫基羰基、正己基硫基羰基、1，1-二甲基丙基硫 基羰基、1，2-二曱基丙基硫基羰基、1-甲基戊基硫基羰 基、2-曱基戊基硫基羰基、3-曱基戊基硫基羰基、4-甲基 戊基硫基羰基、1，1_二曱基丁基硫基羰基、1，2-二甲基丁 基硫基羰基、1，3-二甲基丁基硫基羰基、2,2-二甲基丁基 硫基羰基、2,3-二甲基丁基硫基羰基、3,3-二甲基丁基硫 基羰基、1-乙基丁基硫基羰基、2-乙基丁基硫基羰基、 1，1，2·三曱基丙基硫基羰基、1，2,2-三甲基丙基硫基羰基、 115703.doc -21- 200806642 1-乙基-1-甲基丙基硫基羰基或1-乙基_2_甲基丙基硫基幾 基。 如本文中所使用之術語”Ci-C6烷基亞磺醯基”（Cl-C6烧基 亞颯基· Ci-C6烧基-S(=0)-)係指經由亞續醯基之硫原子鍵 結於烷基中之任一鍵處的具有1至6個碳原子之直鏈或支鏈 飽和烴基（如上文所提及），例如S0_CH3、S〇_C2h5、正丙 基亞磺醯基、1-曱基乙基亞磺醯基、正丁基亞磺醯基、^ 曱基丙基亞石黃醯基、2_甲基丙基亞石黃醯基、ι，ι_二甲基乙 基亞磺醯基、正戊基亞磺醯基、1-曱基丁基亞磺醯基、2_ 甲基丁基亞磺醯基、3-甲基丁基亞磺醯基、^-二甲基丙 基亞磺醯基、1，2-二曱基丙基亞磺醯基、2,2_二甲基丙基 亞磺醯基、1-乙基丙基亞磺醯基、正己基亞磺醯基、丨一甲 基戊基亞石頁醯基、2-甲基戊基亞石黃醯基、3 -甲基戊基亞石黃 醯基、4-甲基戊基亞磺醯基、^^二甲基丁基亞磺醯基、 1，2-二甲基丁基亞磺醯基、二曱基丁基亞磺醯基、2,2-二甲基丁基亞磺醯基、2,3-二甲基丁基亞磺醯基、3，3-二 甲基丁基亞磺醯基、1-乙基丁基亞磺醯基、乙基丁基亞 石黃醯基、1，1，2-三甲基丙基亞磺醯基、三甲基丙基亞 石黃酿基、1-乙基-1-甲基丙基亞磺醯基或丨_乙基_2-曱基丙基 亞石黃醢基。 術語’’CrC6烧基胺基”係指帶有1個如上文所定義之烷基 之第二胺基，例如甲基胺基、乙基胺基、丙基胺基、；μ甲 基乙基胺基、丁基胺基、^甲基丙基胺基、甲基丙基胺 基、1，1-二甲基乙基胺基、戊基胺基、丨—甲基丁基胺基、 115703.doc -22- 200806642 2-曱基丁基胺基、3-甲基丁基胺基、2，2-二甲基丙基胺 基、1-乙基丙基胺基、己基胺基、1，1-二曱基丙基胺基、 1，2 -二甲基丙基胺基、1-甲基戊基胺基、2-甲基戊基胺 基、3 -甲基戊基胺基、4-甲基戊基胺基、1，1_二曱基丁基 胺基、1，2-二甲基丁基胺基、1，3-二曱基丁基胺基、2,2_二 甲基丁基胺基、2，3 -二甲基丁基胺基、3,3 -二甲基丁基胺 基、1-乙基丁基胺基、2-乙基丁基胺基、l，i，2-三甲基丙基 胺基、1，2,2-三甲基丙基胺基、1-乙基4-曱基丙基胺基或 1-乙基-2-甲基丙基胺基。 術$吾π二（C1 - C6燒基）胺基π係指帶有2個如上文所定義之 烷基之第三胺基，例如二甲基胺基、二乙基胺基、二正丙 基胺基、二異丙基胺基、Ν-乙基-Ν-甲基胺基、Ν-(正丙 基）甲基胺基、Ν-(異丙基）-Ν-甲基胺基、Ν-(正丁基 甲基胺基、Ν-(正戊基）_Ν-曱基胺基、Ν-(2-丁基）-Ν-曱基胺 基、Ν-(異丁基）-Ν-曱基胺基、Ν-(正戊基）曱基胺基、 Ν-(正丙基）乙基胺基、Ν-(異丙基）-Ν_乙基胺基、Ν-(正 丁基）-Ν·乙基胺基、Ν-(正戊基）乙基胺基、Ν-(2-丁基）-Ν-乙基胺基、Ν-(異丁基）-Ν-乙基胺基或Ν-(正戊基）-Ν-乙 基胺基。 如本文中所使用之術語”Ci_c6烷基磺醯基”（Ci-C6烷基-S(=0)2·)係指經由磺醯基之硫原子鍵結於烷基中之任一鍵 處的具有1至6個碳原子之直鏈或支鏈飽和烷基（如上文所 提及），例如S02-CH3、S02-C2H5、正丙基磺醯基、s〇2-CH(CH3)2、正丁基磺醯基、i-甲基丙基磺醯基、2·甲基丙 115703.doc -23- 200806642 基磺醯基、S〇2_C(CH3)3、正戊基磺醯基、丨·甲基丁基磺醯 基、2-甲基丁基磺醯基、3-曱基丁基磺醯基、二甲基 丙基％ i&基、1，2-二甲基丙基石黃醯基、2,2-二甲基丙基石黃 醯基、1-乙基丙基磺醯基、正己基磺醯基、“甲基戊基磺 醯基、2-甲基戊基磺醯基、3_甲基戊基磺醯基、4_甲基戊 基石買醯基、1,1-二甲基丁基磺醯基、12-二甲基丁基磺醯 基、1，3-二甲基丁基磺醯基、2,2_二曱基丁基磺醯基、2,3一 二甲基丁基磺醯基、3,3-二甲基丁基磺醯基、^乙基丁基 磺醯基、2-乙基丁基磺醯基、u，2_三甲基丙基磺醯基、 1，2,2-三甲基丙基磺醯基、乙基甲基丙基磺醯基或卜 乙基-2-甲基丙基石黃醯基。 如本文中所使用及在c^c：6烯基氧基、c2-c6烯基胺基、 c2-c6烯基硫基、c2-C6烯基磺醯基、（c2-c6烯基）羰基、 (C^-C：6烯基氧基）羰基及（c^c：6烯基）羰基氧基之烯基部分中 之術語nC2_C6烯基”係指具有2至6個碳原子及在任一位置處 之1個雙鍵之直鏈或支鏈不飽和烴基，諸如乙稀基、丨-丙 烯基、2-丙烯基、1-甲基_乙烯基、丨_丁烯基、2_丁稀基、 3-丁烯基、1-甲基_1_丙烯基、2-甲基_ι_丙稀基、卜甲基_2_ 丙烯基、2-甲基-2-丙烯基、1-戊烯基、2_戊烯基、3_戊烯 基、4-戊烯基' 1-曱基-1_丁稀基、2_甲基•丁烯基、3_甲 基-1-丁烯基、1-曱基-2-丁烯基、2-甲基-2-丁烯基、3-甲 基-2-丁烯基、1-甲基丁烯基、2-甲基-3-丁稀基、3 -甲 基-3-丁烯基、1，1_二甲基_2_丙烯基、二曱基_卜丙烯 基、1，2-二甲基-2-丙稀基、1-乙基-1-丙烯基、丨_乙基_2_丙 115703.doc -24- 200806642 稀基、1-己細基、2-己稀基、3 -己稀基、4-己稀基、5 -己 烯基、1-甲基-1-戊稀基、2-甲基-1·戊稀基、3 -甲基-1·戊 烯基、4-曱基-1-戊烯基、1-甲基-2-戊烯基、2-曱基_2-戊 烯基、3 -甲基-2-戊烯基、4-甲基-2-戊烯基、1-曱基-3-戊 烯基、2-甲基-3-戊烯基、3 -曱基-3-戊烯基、4-曱基-3-戊 烯基、1-曱基-4-戊烯基、2-甲基-4-戊烯基、3-曱基-4-戊 烯基、4-甲基-4·戊烯基、；[，：[_二甲基_2_ 丁烯基、1，1-二甲 基-3-丁烯基、1，2-二甲基-1-丁烯基、ι，2-二甲基-2-丁歸 基、1，2-二甲基-3-丁烯基、ι，3-二甲基-1-丁烯基、1，3_二 甲基-2-丁烯基、1，3-二曱基-3-丁烯基、2,2-二曱基-3-丁烯 基、2,3-二甲基_1_丁烯基、2,3_二甲基_2_丁烯基、2,3_二 甲基-3-丁烯基、3,3-二甲基-1-丁烯基、3,3_二甲基-2-丁歸 基、1-乙基-1-丁烯基' ；[_乙基_2_ 丁烯基、丨_乙基_3_ 丁烯 基、2-乙基-1-丁烯基、2-乙基-2-丁烯基、2-乙基-3-丁烯 基、1，1，2·三甲基-2-丙烯基、^乙基-曱基·2_丙烯基、κ 乙基-2-甲基-1-丙烯基及丨_乙基-2_甲基-2_丙烯基。 如本文中所使用之術語"CrG烯基氧基，，係指經由氧原子 連接之具有2至6個碳原子之直鏈或支鏈飽和烯基（如上文 所提及），諸如乙烯基氧基、烯丙基氧基（丙烯基氧 基）、甲基烯丙基氧基、丁烯_4_基氧基等。 如本文中所使用之術語”CrC6烯基硫基，•係指經由硫原子 連接之具有2至6個碳原子之直鏈或支鏈飽和烯基（如上文 所提及），例如乙烯基硫基、烯丙基硫基（丙烯_3_基硫 基）、甲基烯丙基硫基、丁烯_4_基硫基等。 115703.doc -25· 200806642 如本文中所使用之術語”C2_c0烯基胺基”係指經由胺基連 接之具有2至6個碳原子之直鏈或支鏈飽和烯基（如上文所 提及），例如乙烯基胺基、烯丙基胺基（丙烯基胺基）、 甲基烯丙基胺基、丁烯-4-基胺基等。 如本文中所使用之術語"CrC6烯基磺醯基”係指經由磺醯 基（S〇2)連接之具有2至6個碳原子之直鏈或支鏈飽和烯基 (如上文所提及），例如乙烯基磺醯基、烯丙基磺醯基（丙 烯-3-基磺醯基）、甲基烯丙基磺醯基、丁稀_4_基磺醯基 等。 如本文中所使用及在CrC6炔基氧基、C2_C6炔基胺基、 c2-c6炔基硫基、c2-C6炔基磺醯基、c2-C6炔基羰基、C2- C6炔基氧基羰基及(^-(：6炔基羰基氧基之炔基部分中之術 語’’CrC6炔基”係指具有2至10個碳原子且含有至少一個參 鍵之直鏈或支鏈不飽和烴基，諸如乙炔基、丙-^炔-^ 基、丙-2-炔_1_基、正丁-卜炔_卜基、正丁 _卜炔_3_基、正 丁-1_炔-4-基、正丁-2-炔_1_基、正戊-^炔―^基、正戊 炔-3-基、正戊-1·炔-4-基、正戊_丨_炔_5_基、正戊-2_炔_1β 基、正戊-2-炔_4_基、正戊_2_炔·5_基、弘甲基丁-卜炔_3_ 基、3-甲基丁-1-炔_4_基、正己-^炔-卜基、正己-卜炔」· 基、正己-1-炔-4-基、正己_丨·炔_5_基、正己·卜炔_6_基、 正己-2-炔-1-基、正己_2_炔_4_基、正己_2_炔_5_基、正己_ 2-炔_6_基、正己-3-炔-i•基、正己-3·炔·2_基、弘甲基戊 炔-1-基、3-曱基戊基、3_甲基戊炔_4_基、弘甲 基戊-1-炔-5-基、4-甲基戊_1_炔-基、4_曱基戊_2_炔_4_基 115703.doc -26- 200806642 或4-甲基戊-2-炔-5-基及其類似基團。 如本文中所使用之術語”(VC：6炔基氧基"係指經由氧原子 連接之具有2至6個碳原子之直鏈或支鏈飽和炔基（如上文 所提及），諸如炔丙基氧基（丙炔_3_基氧基）、丁炔_3_基氧 基及丁炔-4-基氧基。 如本文中所使用之術語炔基硫基’·係指經由硫原子 連接之具有2至6個碳原子之直鏈或支鏈飽和炔基（如上文 所提及），諸如炔丙基硫基（丙炔_3_基硫基）、丁炔_3_基硫 基及丁快-4-基硫基。 如本文中所使用之術語"CrC：6炔基胺基π係指經由胺基連 接之具有2至6個碳原子之直鏈或支鏈飽和炔基（如上文所 提及），諸如炔丙基胺基（丙炔_3_基胺基）、丁炔_3_基胺基 及丁快-4 -基胺基。 如本文中所使用之術語"(VC6炔基磺醯基”係指經由磺醯 基（S〇2)連接之具有2至6個碳原子之直鏈或支鏈飽和炔基 (如上文所提及），諸如快丙基續醯基（丙炔基續醯基）、 丁快-3-基續醯基及丁快-4-基續醯基。 如本文中所使用之術§吾nC3-C i2環烧基"係指具有3至12個 石反原子’尤其為3至6個碳原子之單環或雙環或多環烴基。 單環基之實例包括環丙基、環丁基、環戊基、環己基、環 庚基、環辛基、環壬基及環癸基。雙環基之實例包括雙環 [2.2.1] 庚基、雙環[3.1.1]庚基、雙環[2·2·2]辛基及雙環 [3.2.1] 壬基。三環基之實例為金剛烷基及高金剛烷基。 如本文中所使用之術語”單環或雙環雜芳環”係指具有5 115703.doc -27- 200806642 或6個環成員之單環雜芳基，其可包括稠合5員、6員戋7員 環並因此具有8至10個之環成員總數，其中在各狀況下， 該等環成員之1、2、3或4者為彼此獨立地選自由氧、硫、 亂組成之群之雜原子。雜環基可經由碳環成員或經由氮環 成員連接至分子之剩餘部分。稠合環包括烷基、 Cs-C7環烯基或5至7員雜環基及苯基。The sympathomimetic effect of a 2-(1-tetrahydronaphthylamino)-s-porphyrin compound is described in Zasshi (1965), 61(6), pp. 479-89, which describes its vasoconstrictor effect or in US 4,520,014. Its efficacy in nasal compositions is described in Arzneimittelforschung 1962, 12, pp. 975-8. US 2,883,410, US 2,870,161 and US 2,870,159 describe 2-(1-dihydrodecylamino)-oxazoline as a Ningshen in pharmaceutical compositions, the first two of which disclose 2-(4- Thio-t-butyl-indole-dihydroindenylamino> oxazoline. US 2,956,072 discloses 2-(1-tetrahydronaphthylamino)-oxazole, which is used for the same purpose. Oxazoline or imidazoline substituted 2·(1_tetrahydronaphthylamino)-bamboo organism or 2-(1-I-indolylamino)-derivative can be found in us 3,636,219 and 118 3,679,798, which are described Its anti-cholinergic effect. Aryl-amino-oxazoline or aryl-amino-thiazoline has been discussed as an insecticide in _ 丨 丨 963 192 or in DE_b 1 954 584 Discussion of crop protection. None of the latter two documents disclose derivatives which reveal dihydroindenyl- or tetrahydronaphthyl-amino-oxazolines with comparable substitution procedures, in which dihydroindenyl or tetrahydronaphthyl rings The aromatic moiety of the system is substituted. Preferably, the di-nodal or tetrahydronaphthyl-amino-oxazoline is substituted at position A and / or C and / or hydrazine. Preferably, indoline Tetrahydronaphthalene The non-fused portion of the ring system is not retained. 115703.doc 13 200806642 The substituted state and the oxazoline ring system retain the unsubstituted state. The compound of formula I may have one or more pairs of palmar centers, in which case it Isomers or mixtures of stereoisomers of diastereomers are present. The invention provides, for example, pure enantiomers or pure diastereomers of pure diastereomers and mixtures thereof. The compounds of formula 1 may also be different from each other. The form of the isomer is present. The invention includes a single tautomer, if separable, and a mixture of tautomers. According to the invention, the salt of the compound of formula 1 suitable for use is especially agriculturally acceptable. It can be formed by a conventional method, for example, if the formula "the compound has a test "b group, it is formed by reacting a compound with the acid of the anion or by reacting the acidic compound of the formula 1 with a suitable base. Suitable agriculture ± applicable 帛 especially for their cations "salt or their acid 夂 成 1 . 亥 亥 等 cations and _ ions respectively, the role of the compound according to the invention does not have any disadvantage Suitable cations, especially alkali metal ions, are preferably clock, nano and potassium ions; soil metal ions, preferably ruthenium, osmium and iridium ions; and transition metal ions, preferably for identification, copper, and years. And iron ions, as well as sulphur ions (NH4+) and substituted ammonium ions, wherein 1 to 4 of the hydrogen atoms are through Cl-C4 alkyl, Ci_c4 hydroxyalkyl, {decane dairy, eve: 4 alkane Aldo-Cl-C4 alkyl, hydroxy-Ci_C4 alkoxy-Ci-alkanyl, phenyl and/or benzyl are substituted. Examples of substituted ammonium ions include methyl hydrazine ion, isopropyl ammonium ion, Dimethylammonium ion, diisopropylammonium ion, monomethyl phosphonium ion, tetramethylammonium ion, tetraethylammonium ion, tetra-T-ammonium ion, 2-hydroxyethylammonium ion, 2-(2-hydroxyl) Ethoxy)ethyl hydrazine ion, bis(2-hydroxyethyl)ammonium ion, benzyltrimethylammonium ion and benzyl 115703.doc -14 - 200806642 bistriethylammonium ion, in addition to scale ions, strontium ions Preferably, it is a tris(c-C4 alkyl)phosphonium ion and a cerium oxide ion, preferably a tri(Ci_C4 alkyl) oxidizing ion. The anion of the acid addition salt is mainly gas ion, bromide ion, fluoride ion, hydrogen sulfate, sulfate, dihydrogen phosphate, hydrogen phosphate, acid salt, nitrate, hydrogen carbonate, carbonate, hexafluoroantimony. The anion of hexanoate, hexafluorophosphate, benzoate and C^C:4 alkanoic acid is preferably citrate, acetate, propionate and butyrate. It can be formed by reacting a compound of the formula with an acid of the corresponding anion, preferably hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid or nitric acid. Similar to the term halogen, the organic part referred to in the definition of the above variables is a collective term for individual lists of individual group members. In each case, the prefix cn-cm indicates the possible number of carbon atoms in the group. In each case the term halogen means fluorine, bromine, gas or iodine, especially fluorine, gas or moisture. Examples of other meanings are: as used herein and in (^-(^ alkoxy, ^-〇6 alkylamino, bis(CVC6 alkyl)amine, CVC6 alkylthio, CVC6 alkyl sulfonate The term "C" in the alkyl portion of a fluorenyl group, a CV C6 alkyl group, a Cl_c6 alkylcarbonyl group, a Cl_c6 alkoxycarbonyl group, a Cl-C6 alkylthiocarbonyl group, and a CrC6 alkylcarbonyloxy group. "Acrylate" means a radical having from 1 to 6 carbon atoms, a saturated linear or branched hydrocarbon group, especially 1 to 4 carbons, such as methyl, ethyl, propyl ' κ methyl ethyl, butyl , 1-methylpropyl, methyl propyl, dimethylethyl, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 2, 2, 115,703. Doc •15· 200806642 Dimercaptopropyl, 1-ethylpropyl, hexyl, 1,1-dimethylpropyl, 1,2-dimercaptopropyl, 1-methylpentyl, 2-methyl Pentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-didecylbutyl, 1,3,dimethylbutyl, 2, 2-dimethylbutyl, 2,3-dimethylbutyl, 3,3·didecylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2·trimethyl Propyl group 2,2·trimethylpropyl, 1-ethyl-1-methylpropyl, 1-ethyl-2-methylpropyl, heptyl, octyl, 2-ethylhexyl, decyl and hydrazine And its isomer. Cl-C4 alkyl means, for example, methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl or 1,1-Dimethylethyl. The term "CrC6 haloalkyl" as used herein refers to a straight or branched saturated alkyl group having one carbon atom (as mentioned above), wherein Some or all of the hydrogen atoms in the group may be replaced by a functional atom as mentioned above, such as a CrC4 haloalkyl group such as chloromethyl, bromomethyl, di-methylmethyl, trichloromethyl, fluoromethyl. , difluoromethyl, trifluoromethyl, fluorofluorenyl, difluorofluoromethyl, chlorodifluoromethyl, 1 · chloroethyl; [• desert ethyl, fluoroethyl, 2-fluoroethyl Base, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 2-gas-2.fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-di Chloro-2-fluoroethyl, 2,2,2-trichloroethyl, pentafluoroethyl and the like. The term "C-C6 alkoxy" as used herein refers to via oxygen A straight-chain or branched saturated alkyl group having 1 to 6 carbon atoms (as mentioned above) is attached. Examples include Ci-C6 alkoxy groups such as methoxy, ethoxy, OCH2-C2H5, hydrazine CH(CH3)2, n-butoxy' 〇CH(CH3)-C2H5, OCH2-CH(CH3)2, oc(ch3)3, n-pentyloxy, benzyloxy, 2-methylbutoxy , 3-methylbutoxy, i, bis dimethylpropoxy, i, 孓 2,115,703.doc -16· 200806642 methyl propenyl, 2,2-dimethyl-propoxy, ethyl ethyl Oxyl, n-hexyloxy, 1-methylpentyloxy, 2-methylpentyloxy, 3-methylpentyloxy, 4-methylpentyloxy, 1,1-dimethylbutoxy, ! ,> dimethylbutoxy,! , Hong Di-Butyloxy, 2,2-dimethylbutoxy, 2,3-dimercaptobutoxy, 3,3-didecylbutoxy, 1-ethylbutoxy, 2 _Ethyl butoxy group, trimethylpropoxy group, 1,2,2-trimethylpropoxy group, ethylidene-1-mercaptopropoxy group, 1-ethyl-2-fylpropoxy group and Its similar group. The term "CrQ haloalkoxy" as used herein refers to a CrC6 alkoxy group as mentioned above, wherein a hydrogen atom is partially or completely substituted by fluorine, chlorine, bromine and/or iodine, that is, for example, Cl_C6. Haloalkoxy, such as chloromethoxy, dichloromethoxy, trichloromethoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, fluoromethoxy, difluorocarbon Oxy, chlorodifluoromethoxy, 2·fluoroethoxy, 2-oxoethoxy, 2-bromoethoxy, 2-Ethyloxy, 2,2-difluoroethoxy, 2, 2,2-trifluoroethoxy, 2-chloro-2-fluoroethoxy, 2-gas-2,2-difluoroethoxy, 2,2-dichloro-2-fluoroethoxy, 2 , 2,2-trichloroethoxy, pentafluoroethoxy, 2-fluoropropoxy, 3-fluoropropoxy, 2,2 difluoropropoxy, 2,3-difluoropropoxy, 2_chloropropoxy, % chloropropoxy, 2,3-dipropoxy, 2-bromopropoxy, 3-bromopropoxy, 3,3,3-trifluoropropoxy, 3 , 3,3-trichloropropoxy, 2,2,3,3,3-pentafluoropropoxy, hexafluoropropoxy, 1·(fluoromethyl)-2-fluoroethoxy, _(gas methyl)_2·chloroethoxy, W desert methyl)-2- ethoxyethoxy, 4-fluorobutoxy, cardiobutoxy, 4-bromobutoxy, nonafluorobutoxy , 5-fluoro-indolyl pentyloxy 5 qi-1-pentyloxy, yl, yl, 5-indol-1-pentyloxyundecyloxy-inden-1-pentyloxy, 5,5 , 5_three gas • pentyloxy 6-chloro-1-hexyloxy, 6_ 115703.doc -17- 200806642 1 ^ hexyloxy, 6-fluorene]-hexyloxy, 6, m_trichloromethane Or a dodecafluorohexyloxy group, especially chloromethoxy, fluoromethoxy, 2-methoxymethoxy, trifluoromethoxy, 2-fluoroethoxy, 2·chloroethoxy or 2,2 , 2_trifluoroethoxy. The term "Cl_C6 alkoxy^alkyl" as used herein refers to an alkyl group wherein one carbon atom carries one alkoxy group as mentioned above. Examples are CH^OCH3, CH2-OC2H5 , n-propoxymethyl, CH2-OCH(CH3)2, n-butoxymethyl, (1-methylpropoxy)methyl, (21-propoxy)methyl, CH2_0C(CH3)3 , 2-((methoxy)ethyl, (ethoxy)ethyl, 2-(n-propoxy)ethyl, 2-(b-methylethoxy)ethyl, 2-(n-butoxy)ethyl , 2-(1-methylpropoxy)ethyl, 2-methylpropoxy)ethyl, 2-(1,1·dimethylethoxy)ethyl, 2-(methoxy)propyl , 2-(ethoxy)propyl, 2-(n-propoxy)propyl, 2-((methylethoxy)propyl, 2-(n-butoxy)propyl, 2_〇-methylpropoxy Propyl, 2-(2-methylpropoxy)propyl, 2-(u-dimethylethoxy)propyl, %(methoxy)propyl, 3-(ethoxy)propyl , 3-(n-propoxy)propyl, 3-(1-methylethoxy)propyl, 3-(n-butoxy)propyl, 3-(1-methylpropoxy)propyl, 3-(2-methylpropoxy)propyl, ^, hexane Ethoxy)propyl, 2-(methoxy)butyl, 2-(ethoxy)butyl, 2-(n-propoxy)butyl, 2·(1-methylethoxy)butyl, 2_(n-butoxy)butyl, 2-(1-methylpropoxy)butyl, 2-(2-methylpropoxy)butyl, 2-(1,b-dimethylethoxy)butyl , 3-((methoxy)butyl, 3-(ethoxy)butyl, 3-(n-propoxy)butyl 3(1-methylethoxy)butyl, 3-(n-butoxy) Butyl, methylpropoxy)butyl, methylpropoxy)butyl, 3-(1,1-dimethylethoxy)butyl, 4-(methoxy)butyl, 4_(ethoxy)butyl, 4•(n-propoxy) 115703.doc •18- 200806642 Butyl, 4-(1-methylethoxy)butyl, 4-(n-butoxy)butyl Base, 4-(p-methylpropoxy)butyl, 4-(2-methylpropoxy)butyl, '(ij•didecylethoxy)butyl and the like. The term "(Cl-C0 alkyl)carbonyl" as used herein refers to a straight or branched saturated alkyl group having from 1 to 6 carbon atoms bonded to any of the bonds in the alkyl group via a carbonyl group. Mentioned) Examples include Ci_C6 alkylcarbonyl such as CO-CH3, CO-C2H5, n-propylcarbonyl, fluorenyl-methylethyl rotyl, n-butyl, 1-methylpropyl, 2-methyl Propyl, di-decylethylcarbonyl, n-pentylcarbonyl, 1-decylbutylcarbonyl, 2-methylbutylcarbonyl, 3-methylbutylcarbonyl, 1,1-dimethylpropylcarbonyl 1,2-dimethylpropylcarbonyl, 2,2-dimercaptopropylcarbonyl, 1-ethylpropylcarbonyl, n-hexylcarbonyl, 1-methylpentylcarbonyl, 2-methylpentylcarbonyl , 3-methylpentylcarbonyl, 4-methylpentylcarbonyl, 1,1-dimethylbutylcarbonyl, 1,2-didecylbutylcarbonyl, I% dimethylbutylcarbonyl, 2,2 _Dimethylbutylcarbonyl, 2,3-dimethylbutylcarbonyl, 3,3-dimethylbutylcarbonyl, 1-ethylbutylcarbonyl, 2-ethylbutylcarbonyl, l,i, 2-trimethylpropylcarbonyl, 1'2,2-dimethylpropyl, 1-ethyl-1-methylpropyl or iota-2-methylpropylcarbonyl Its similar group. The term "(CVC6 alkoxy)carbonyl, as used herein, refers to a straight or branched alkoxy group having from 1 to 6 carbon atoms attached through a carbon atom of a carbonyl group (as mentioned above), For example, co-och3, CO-OC2H5, coo-ch2-C2H5, CO-OCH(CH3)2, n-butoxymethyl, CO-OCHCCl·^)-c2H5, c〇-och2-ch(ch3)2 CO-OC(CH3)3, n-pentyloxycarbonyl, 1-methylbutoxycarbonyl, 2-methylbutoxycarbonyl, 3-methylbutoxy 115703.doc -19- 200806642 BASE, 2 ,2-dimethylpropoxycarbonyl, puethylpropoxycarbonyl, n-hexyloxycarbonyl, dimethylpropoxycarbonyl, U2_dimethylpropoxylopyryl, 1-methylpentyloxycarbonyl , 2-methylpentyloxycarbonyl, 3-methylpentyloxycarbonyl, 4-methylpentyloxycarbonyl, anthracene, bisdimethylbutoxycarbonyl, 1,2-dimethylbutoxycarbonyl , 13-dimethylbutoxycarbonyl, 2,2-dimethylbutoxycarbonyl, 2,3-dimethylbutoxycarbonyl, 3,3-dimethylbutoxycarbonyl, 1-B Butyloxycarbonyl, ethylbutoxycarbonyl, hydrazine, 12-trimethylpropoxycarbonyl, 1,2,2-trimethylpropoxy Base, 丨-ethyl·丨_methylpropoxycarbonyl or 1-ethyl-2-methylpropoxycarbonyl. The term "(Cl-C6 alkyl)carbonyloxy" as used herein. Means a linear or branched saturated alkyl group having from 丨 to 6 carbon atoms (as mentioned above) bonded to any of the bonds through a carbon atom of a carbonyloxy group, such as 〇_CO-CH3, 〇弋0-(:5, n-propylcarbonyloxy, benzylethylcarbonyloxy, n-butylcarbonyloxy, 丨-methylpropylcarbonyloxy, 2-mercaptopropyloxy 1,1·Dimethylethylcarbonyloxy, n-pentylcarbonyloxy, 1-methylbutylcarbonyloxy, 2-methylbutylcarbonyloxy, hydroxymethylbutyloxy 1,1·Dimethylpropylcarbonyloxy or 1>2-dimethylpropylcarbonyloxy. The term "〇1-(:6 alkylthio) (Cl-c6 alkane) as used herein. Alkylthio:CrC6alkyl-S-)" means a straight or branched saturated alkyl group having 1 to 6 carbon atoms (as mentioned above), such as a thio group, such as a thiol group, which is bonded via a sulfur atom, such as Methylthio, ethylthio, propylthio, fluorenyl Ethylthio, butylthio, 1-methylpropylthio, 2-methylpropylthio, 1,1·dimethylethylthio, n-pentylthio, 1-methyl Butylthio, 2_115703.doc -20- 200806642 nonylbutylthio, 3-methylbutylthio, 2,2-dimercaptopropylthio, 1-ethylpropylthio, n-Hexylthio, 1,1-dimethylpropylthio, anthracene, 2-diisopropylpropylthio, 1-methylpentylthio, 2-decylpentylthio, 3-methyl Amylthio, 4-methylpentylthio, iota, dimethyl dimethylthio, 1,2-dimethylbutylthio, iota, 3-dimethylbutylthio 2,2-Dimethylbutylthio, 2,3-dimethylbutylthio, 3,3-dimethylbutylthio, 1-ethylbutylthio, 2-ethyl Butylthio, l,i,2-trimethylpropylthio, 1,2,2-dimercaptopropylthio, 1-ethyl-1-methylpropylthio or 1 -B Base 2 -methylpropylthio. The term "(CrG alkylthio)carbonyl" as used herein refers to a straight or branched alkylthio group having from 1 to 6 carbon atoms attached via a carbon atom of a carbonyl group (as mentioned above) and). Examples include CO-SCH3, CO-SC2H5, CO_SCH2-C2H5, CO-SCH(CH3)2, n-butylthiocarbonyl, co-SCH(CH3)-C2H5, CO-SCH2-CH(CH3)2, CO- SC(CH3)3, n-pentylthiocarbonyl, 1-methylbutylthiocarbonyl, 2-methylbutylthiocarbonyl, 3-methylbutylthiocarbonyl, 2,2-dimethyl Propylthiocarbonyl, 1-ethylpropylthiocarbonyl, n-hexylthiocarbonyl, 1,1-dimethylpropylthiocarbonyl, 1,2-dimercaptopropylthiocarbonyl, 1- Methyl amylthiocarbonyl, 2-mercaptoylthiocarbonyl, 3-mercaptoylthiocarbonyl, 4-methylpentylthiocarbonyl, 1,1-didecylbutylthiocarbonyl 1,2-dimethylbutylthiocarbonyl, 1,3-dimethylbutylthiocarbonyl, 2,2-dimethylbutylthiocarbonyl, 2,3-dimethylbutylsulfur Carbocarbonyl, 3,3-dimethylbutylthiocarbonyl, 1-ethylbutylthiocarbonyl, 2-ethylbutylthiocarbonyl, 1,1,2·trimercaptopropylthiocarbonyl 1,2,2-Trimethylpropylthiocarbonyl, 115703.doc -21- 200806642 1-Ethyl-1-methylpropylthiocarbonyl or 1-ethyl-2-methylpropylsulfide Base several bases. The term "Ci-C6 alkylsulfinyl" (C1-C6 alkylsulfinyl-Ci-C6 alkyl-S(=0)-) as used herein refers to sulfur via a sub-continuous sulfhydryl group. a linear or branched saturated hydrocarbon group having 1 to 6 carbon atoms bonded to any of the alkyl groups (as mentioned above), for example, S0_CH3, S〇_C2h5, n-propylsulfinyl, 1-mercaptoethylsulfinyl, n-butylsulfinyl, hydrazinopropyl sulphate, 2-methylpropyl sulphate, iota, dimethyl sulfinium , n-pentylsulfinyl, 1-mercaptobutylsulfinyl, 2-methylbutylsulfinyl, 3-methylbutylsulfinyl, ^-dimethylpropyl Sulfonyl, 1,2-dimercaptopropylsulfinyl, 2,2-dimethylpropylsulfinyl, 1-ethylpropylsulfinyl, n-hexylsulfinyl,丨Methylpentyl sulfite, 2-methylpentyl sulphate, 3-methylpentyl sulphate, 4-methylpentyl sulfinyl, ^^ dimethyl butyl Sulfosyl, 1,2-dimethylbutylsulfinyl, dimercaptobutylsulfinyl, 2,2-dimethylbutylsulfinyl 2,3-Dimethylbutylsulfinyl, 3,3-dimethylbutylsulfinyl, 1-ethylbutylsulfinyl, ethylbutyl sulfite, 1,1 , 2-trimethylpropylsulfinyl, trimethylpropyl sulfite, 1-ethyl-1-methylpropylsulfinyl or 丨_ethyl_2-mercaptopropyl Kea stone scutellaria. The term ''CrC6 alkylamino group' refers to a second amine group having one alkyl group as defined above, such as methylamino, ethylamino, propylamino, μmethylethyl Amino, butylamino, methylpropylamino, methylpropylamino, 1,1-dimethylethylamino, pentylamino, fluorenyl-methylbutylamino, 115703 .doc -22- 200806642 2-Mercaptobutylamino, 3-methylbutylamino, 2,2-dimethylpropylamino, 1-ethylpropylamino, hexylamino, 1 , 1-dimercaptopropylamino, 1,2-dimethylpropylamino, 1-methylpentylamino, 2-methylpentylamino, 3-methylpentylamino, 4-methylpentylamino, 1,1 -didecylbutylamino, 1,2-dimethylbutylamino, 1,3-didecylbutylamino, 2,2_2 Methylbutylamino, 2,3-dimethylbutylamino, 3,3-dimethylbutylamino, 1-ethylbutylamino, 2-ethylbutylamino, l ,i,2-trimethylpropylamino, 1,2,2-trimethylpropylamino, 1-ethyl 4-mercaptopropylamino or 1-ethyl-2-methylpropane Amino group. 吾π二(C1 - C6 alkyl) amine π Refers to a third amine group having two alkyl groups as defined above, such as dimethylamino, diethylamino, di-n-propylamino, diisopropylamino, oxime-ethyl- Ν-Methylamino, Ν-(n-propyl)methylamino, Ν-(isopropyl)-oxime-methylamino, Ν-(n-butylmethylamino, Ν-(n-pentyl) _Ν-mercaptoamine, Ν-(2-butyl)-fluorenyl-mercaptoamine, Ν-(isobutyl)-fluorenyl-fluorenylamino, fluorenyl-(n-pentyl) decylamino, Ν-(n-propyl)ethylamino, Ν-(isopropyl)-oxime-ethylamino, Ν-(n-butyl)-oxime ethylamino, Ν-(n-pentyl) Amino group, Ν-(2-butyl)-fluorene-ethylamino group, fluorenyl-(isobutyl)-fluorene-ethylamino group or fluorenyl-(n-pentyl)-fluorene-ethylamino group. The term "Ci_c6 alkylsulfonyl" (Ci-C6 alkyl-S(=0)2.) as used herein refers to having a bond to a sulfur atom of a sulfonyl group bonded to any of the alkyl groups. a linear or branched saturated alkyl group of 1 to 6 carbon atoms (as mentioned above), for example, S02-CH3, S02-C2H5, n-propylsulfonyl, s〇2-CH(CH3)2, positive Butylsulfonyl, i-methylpropylsulfonyl, 2·methyl 115703.doc -23- 200806642 sulfenyl, S〇2_C(CH3)3, n-pentylsulfonyl, fluorenylmethylbutylsulfonyl, 2-methylbutylsulfonyl, 3-hydrazine Butyl sulfonyl, dimethylpropyl% i& base, 1,2-dimethylpropyl sulphate, 2,2-dimethylpropyl sulphate, 1-ethylpropyl sulfonyl, hexyl Sulfosyl, "methylpentylsulfonyl, 2-methylpentylsulfonyl, 3-methylpentylsulfonyl, 4-methylpentylstone, decyl, 1,1-dimethyl Butylsulfonyl, 12-dimethylbutylsulfonyl, 1,3-dimethylbutylsulfonyl, 2,2-didecylbutylsulfonyl, 2,3-dimethyl Butyl sulfonyl, 3,3-dimethylbutylsulfonyl, ethyl butyl sulfonyl, 2-ethylbutyl sulfonyl, u, 2-trimethyl propyl sulfonate Base, 1,2,2-trimethylpropylsulfonyl, ethylmethylpropylsulfonyl or ethyl-2-methylpropyl sulphate. As used herein and in c^c:6 alkenyloxy, c2-c6 alkenylamino, c2-c6 alkenylthio, c2-C6 alkenylsulfonyl, (c2-c6 alkenyl)carbonyl , (C^-C:6 alkenyloxy)carbonyl and the term nC2_C6 alkenyl in the alkenyl moiety of (c^c:6 alkenyl)carbonyloxy means having 2 to 6 carbon atoms and in either a linear or branched unsaturated hydrocarbon group of one double bond at a position, such as ethylene, fluorenyl-propenyl, 2-propenyl, 1-methyl-vinyl, fluorene-butenyl, 2-butadiene , 3-butenyl, 1-methyl-1-propenyl, 2-methyl-I-propyl-propyl, 2-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl , 2-pentenyl, 3-pentenyl, 4-pentenyl ' 1-indenyl-1 -butylenyl, 2-methylbutenyl, 3-methyl-1-butenyl, 1-mercapto-2-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1-methylbutenyl, 2-methyl-3-butene , 3-methyl-3-butenyl, 1,1-dimethyl-2-propenyl, diindenyl-bupropenyl, 1,2-dimethyl-2-propanyl, 1- Ethyl-1-propenyl, 丨_ethyl_2_propene 115703.doc -24- 200806642 dilute base, 1-hexyl base, 2- Dilute, 3-hexyl, 4-hexyl, 5-hexenyl, 1-methyl-1-pentyl, 2-methyl-1.pentyl, 3-methyl-1 Pentenyl, 4-mercapto-1-pentenyl, 1-methyl-2-pentenyl, 2-mercapto-2-pentenyl, 3-methyl-2-pentenyl, 4- Methyl-2-pentenyl, 1-decyl-3-pentenyl, 2-methyl-3-pentenyl, 3-mercapto-3-pentenyl, 4-mercapto-3-pentyl Alkenyl, 1-mercapto-4-pentenyl, 2-methyl-4-pentenyl, 3-mercapto-4-pentenyl, 4-methyl-4.pentenyl, [, :[_Dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-1-butenyl, iota,2-dimethyl-2- Butyl, 1,2-dimethyl-3-butenyl, iota, 3-dimethyl-1-butenyl, 1,3-dimethyl-2-butenyl, 1,3- Dimercapto-3-butenyl, 2,2-dimercapto-3-butenyl, 2,3-dimethyl-1-butenyl, 2,3-dimethyl-2-butene Base, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl, 3,3-dimethyl-2-butylenyl, 1-ethyl-1 -butenyl'; [_ethyl-2-butenyl, 丨_ethyl_3_butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2- Ethyl-3-butenyl 1,1,2·Trimethyl-2-propenyl, ethyl-indenyl-2-propenyl, κethyl-2-methyl-1-propenyl and 丨_ethyl-2_A Base-2_propenyl. The term "CrGalkenyloxy, as used herein, refers to a straight or branched saturated alkenyl group having 2 to 6 carbon atoms attached through an oxygen atom (as mentioned above), such as a vinyl group. An oxy group, an allyloxy group (propyleneoxy group), a methallyloxy group, a butene-4-yloxy group, or the like. The term "CrC6 alkenylthio" as used herein, refers to a straight or branched chain saturated alkenyl group (as mentioned above) having 2 to 6 carbon atoms attached via a sulfur atom, such as vinyl sulphide. Base, allylthio (propylene_3_ylthio), methallylthio, butene-4-ylthio, etc. 115703.doc -25· 200806642 The term as used herein" C2_c0 alkenylamino" means a straight or branched saturated alkenyl group having 2 to 6 carbon atoms attached via an amine group (as mentioned above), for example, a vinylamino group, an allylamino group (propylene) Alkyl), methallylamino, buten-4-ylamino, etc. The term "CrC6 alkenylsulfonyl" as used herein refers to via a sulfonyl group (S〇2). a straight or branched saturated alkenyl group having 2 to 6 carbon atoms (as mentioned above), such as vinylsulfonyl, allylsulfonyl (propen-3-ylsulfonyl), Methylallylsulfonyl, butyryl-4-ylsulfonyl and the like. As used herein and in CrC6 alkynyloxy, C2_C6 alkynylamino, c2-c6 alkynylthio, c2-C6 alkynylsulfonyl, c2-C6 alkynylcarbonyl, C2-C6 alkynyloxy The carbonyl group and the term ''CrC6 alkynyl group' in the alkynyl moiety of the 6-alkynylcarbonyloxy group mean a straight or branched chain unsaturated hydrocarbon group having 2 to 10 carbon atoms and containing at least one reference bond. , such as ethynyl, propyl-propyne-yl, prop-2-yn-1-yl, n-butyl-bupropenyl, n-butyl-butyne-3-yl, n-butyl-1-yne-4 -yl, n-but-2-yne-1_yl, n-pentyl-^-alkynyl, n-pentyn-3-yl, n-pent-1-en-4-yl, n-pentyl-nonyl-alkyne-5 _ base, n-pent-2-ynyl-1β group, n-pent-2-yne-4_yl, n-pent-2-enyne·5_yl, hong methylbut-butyne_3_yl, 3-methyl But-1-yne 4_yl, n-hexyl-^-alkyn-buyl, n-hexan-propyne-yl, n-hex-1-yn-4-yl, n-hexanyl-alkynyl-5-yl, n-hexanyl _6_yl, n-hexan-2-yn-1-yl, n-hexan-2-alkyn-4-yl, n-hexan-2-alkyn-5-yl, n-hexyl-2-ynyl-6-yl, n-hex-3-yne -i•基,正己-3·yne·2_yl, hong methylpentyne-1-yl, 3-mercaptopentyl, 3-methylpentyne _4_yl, hong methyl pentene-1- -5-yl, 4-methylpenta-1-alkynyl, 4-fluorenyl-2-alkyne-4-yl 115703.doc -26- 200806642 or 4-methylpent-2-yne-5- And the like. The term "VC:6 alkynyloxy" refers to a straight or branched saturated alkynyl group having 2 to 6 carbon atoms attached via an oxygen atom (as above Mentioned herein, such as propargyloxy (propyne-3-yloxy), butyne-3-yloxy and butyn-4-yloxy. The term alkynyl as used herein. Sulfur-based refers to a straight or branched saturated alkynyl group having 2 to 6 carbon atoms attached via a sulfur atom (as mentioned above), such as propargylthio (propyne-3-ylthio) And butyne _3_ylthio and butyl-4-ylthio. The term "CrC:6 alkynylamino π as used herein means having 2 to 6 carbons via an amine linkage. a linear or branched saturated alkynyl group of an atom (as mentioned above), such as propargylamino (propyne-3-ylamino), butyne-3-ylamino and butan-4-yl Amine. The term "(VC6 alkynylsulfonyl) as used herein refers to a link through a sulfonyl group (S〇2). a linear or branched saturated alkynyl group having 2 to 6 carbon atoms (as mentioned above), such as a fast-propyl sulfonyl group (propynyl fluorenyl), a di-anthracen-3-yl fluorenyl group And 1,4- 醯 基 。 。 。 。 。 。 n § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § § A cyclic or bicyclic or polycyclic hydrocarbon group. Examples of the monocyclic group include a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, a cycloheptyl group, a cyclooctyl group, a cyclodecyl group, and a cyclodecyl group. Examples of bicyclic groups include bicyclo [2.2.1] heptyl, bicyclo [3.1.1] heptyl, bicyclo [2·2·2] octyl and bicyclo [3.2.1] fluorenyl. Examples of tricyclic groups are adamantyl and high adamantyl. The term "monocyclic or bicyclic heteroaryl ring" as used herein refers to a monocyclic heteroaryl having 5 115703.doc -27-200806642 or 6 ring members, which may include a fused 5 member, 6 member 戋The 7-membered ring and thus has a total number of 8 to 10 ring members, wherein in each case, 1, 2, 3 or 4 of the ring members are independently selected from the group consisting of oxygen, sulfur, and chaos. atom. The heterocyclyl can be attached to the remainder of the molecule via a carbocyclic member or via a nitrogen ring member. The fused ring includes an alkyl group, a Cs-C7 cycloalkenyl group or a 5- to 7-membered heterocyclic group and a phenyl group.

單環5至6員雜芳環之實例包含三嗪基、吡嗪基、嘧啶 基、噠嗪基、吡啶基、噻吩基、呋喃基、吡咯基、啦唑 基、咪唑基、***基、四唑基、噻唑基、噁唑基、噻二唑 基、嗔二唑基、異噻唑基及異噁唑基。 帶有祠合苯環之5員至6員雜芳環之實例為喹啉基 (qumolinyl)、異喹啉基、吲哚基、吲嗪基、異吲哚基、吲 唑基、苯并呋喃基、苯并噻吩基、苯并[b]噻唑基、苯并噁 唑基、苯并噻唑基、苯并噁唑基及苯并咪唑基。帶有稠合 環烯基環之5員至6員雜芳環之實例為二氫吲哚基、二氫吲 秦土 一氫異ϋ引0木基、二鼠啥琳基（dihydrochinolinyl)、二 氫異喹啉基、咣烯基（chromenyl)、咣烷基（chromanyl)及其 類似基團。 術邊’’5至7員雜環基”包括如上文所定義之單環雜芳環及 具有5個、6個或7個環成員之非芳族飽和或部分不飽和雜 衣 非方知J衣之實例包含σ比洛咬基、吼唆琳基、咪嗤琳 基、ϋ比略琳基、吡唑啉基、咪唑啉基、四氫呋喃基、二氫 夫南基 1，3_ 一氣戊環基、二氧雜戊浠基（dioxolenyl)、硫 味基、二氫噻吩基、噁唑啶基、異噁唑啶基、噁唑啉基、 115703.doc -28· 200806642 ^ 琳基、嗟σ坐琳基、異°塞°坐琳基、°塞嗤唆基、異售〇坐 啶基、氧雜硫味基、哌啶基、哌嗪基、哌喃基、二氫哌喃 土 氧辰喃基、一氧°惡烧基、π塞喃基、二氫嗟喃基、四 氮售喃基、嗎啉基、噻嗪基及其類似基團。 . 關於式1化合物之殺蟲活性，較佳者為彼等式I化合物， 其中纟交數彼此獨立地或與其他變數之任一者組合可具有以 下含義： 式1之二氫茚基-或四氫萘基_胺基-唑啉化合物，其中 R1係選自氫、氰基、c(=o)r1c、Cl_C6烷基、（^匕烯 基、CrC6块基、eve：8環烧基、烧氧基，且其中Rlc 係選自氫、CVC6烷基、c2-c6烯基、C2_C6炔基、c3-c8環 烷基、（^-(^烷氧基、（C「C6烷基）胺基、二（Ci-C6烷基）胺 基本基及可為含有1個、2個、3個或4個選自〇、S及N之 雜原子之單環或雙環5至1 〇員雜芳環的雜芳基。 更佳地，式I之二氫茚基-或四氫萘基-胺基·唑啉化合 物，其中R1為氫。 式I之二氫茚基-或四氫萘基-胺基_唑啉化合物，其中仏2 係選自氰基、疊氮基、鹵素、〇H、SH、NH2、CONH2、 S03H、COOH、C(=0)R2e、Cl.c6烧基、c2_c6烯基、C2_C6 炔基、CVC8環烧基、Ci-C6烷氧基、（Ci-C6烧基）胺基、二 (Ci-C6烧基）胺基，其中上述基團之脂族基團中之碳原子可 帶有1個、2個或3個彼此獨立地選自由以下基團組成之群 之基團的任一組合：i素、氰基、硝基、羥基、胺基、羧 基、CVC6烧基、CVC6烧氧基、c2_c6烯基氧基、C2&块 115703.doc -29- 200806642 基氧基、（VC6鹵烷氧基，且其中R2。係選自氫、Ci_c6^ 基、C2-C6烯基、C2-C6炔基、C3-C8環烷基、（^(：6烷氧 基、（CrC6烷基）胺基、二（Ci-C6烷基）胺基、苯基及可為含 有1個、2個、3個或4個選自0、s及N之雜原子之單環或雙 環5至10員雜芳環的雜芳基。 更仏地，式1^--氣節基-或四氫奈基_胺基-唾琳化合 物’其中r係選自鹵素、C^_c6烧基、C2-C6烯基、C2-C6炔 基、Ci-C6烷氧基或CrC：8環烷基，其中該等基團可未經取 代，部分或全部經齒化。 式I之一氫知基或四氫萘基-胺基-唆淋化合物，其中❿為 3且R在位置A、C及D處係經取代。 式I之二氫茚基·或四氫萘基_胺基-唑啉化合物，其中瓜為 2且R2在位置A及C處係經取代。 式I之二氫茚基-或四氫萘基-胺基-唑啉化合物，其中瓜為 2且R2在位置C及D處係經取代。 式I之二氫茚基-或四氫萘基-胺基-唑啉化合物，其中㈤為 1且R2在位置A處係經取代。 式I之二氫茚基·或四氫萘基-胺基-嗤琳化合物，其中瓜為 1且R2在位置C處係經取代。 式I之二氫茚基-或四氫萘基-胺基-唑琳化合物，其中X為 S或0。 式I之二氫茚基-或四氫萘基-胺基·唑琳化合物，其中X為 S ° 較佳者為η為1之式I之二氫節基-胺基_唑啉化合物。 115703.doc -30- 200806642 本發明之化合物可（例如）藉由以下流程中所概括之合成 路線自相應胺II來製備：Examples of monocyclic 5- to 6-membered heteroaryl rings include triazinyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, imidazolyl, triazolyl, Tetrazolyl, thiazolyl, oxazolyl, thiadiazolyl, oxadiazolyl, isothiazolyl and isoxazolyl. Examples of 5- to 6-membered heteroaryl rings with a fluorene ring are qumolinyl, isoquinolyl, indolyl, pyridazinyl, isodecyl, oxazolyl, benzofuran. A benzothiophenyl group, a benzo[b]thiazolyl group, a benzoxazolyl group, a benzothiazolyl group, a benzoxazolyl group, and a benzimidazolyl group. Examples of 5- to 6-membered heteroaryl rings with a fused cycloalkenyl ring are dihydroindenyl, dihydroanthracene, monohydroisoindole, 0-base, dihydrochinolinyl, Hydrogen isoquinolyl, chromenyl, chromanyl and the like. The '5 to 7 membered heterocyclic group' includes a monocyclic heteroaryl ring as defined above and a non-aromatic saturated or partially unsaturated smear having 5, 6 or 7 ring members. Examples of clothing include σ piroxime, fluorene, imiline, oxabendyl, pyrazolinyl, imidazolinyl, tetrahydrofuranyl, dihydroflamyl 1,3_monopentayl , dioxolenyl, thiol, dihydrothienyl, oxazolidinyl, isoxazolidinyl, oxazolinyl, 115703.doc -28· 200806642 ^ Linji, 嗟σ sit琳基,异°塞°坐琳基,°塞嗤唆基, iso-sodium pyridine, oxasulfanyl, piperidinyl, piperazinyl, piperidyl, dihydropiperazin a group, an oxygen group, a oxazide group, a π-mesanyl group, a dihydrofuranyl group, a tetrazirdanyl group, a morpholinyl group, a thiazinyl group and the like. About the insecticidal activity of the compound of the formula 1, Preferred are the compounds of the formula I, wherein the hydrazine number, in combination with each other or with any of the other variables, may have the following meanings: Dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula 1 ,its R1 is selected from the group consisting of hydrogen, cyano, c(=o)r1c, Cl_C6 alkyl, (^, alkenyl, CrC6, eve: 8 cycloalkyl, alkoxy, and wherein Rlc is selected from hydrogen, CVC6 Alkyl, c2-c6 alkenyl, C2_C6 alkynyl, c3-c8 cycloalkyl, (^-(^ alkoxy, (C"C6 alkyl)amino, bis(Ci-C6 alkyl)amine basic group) And may be a heteroaryl group containing 1, 2, 3 or 4 monocyclic or bicyclic 5 to 1 member heteroaryl rings selected from the group consisting of a hetero atom of fluorene, S and N. More preferably, the formula I a dihydroindenyl- or tetrahydronaphthyl-aminoxozoline compound, wherein R1 is hydrogen. A dihydroindenyl- or tetrahydronaphthyl-aminoxozoline compound of the formula I, wherein the oxime 2 is selected from Cyano, azido, halogen, hydrazine H, SH, NH2, CONH2, S03H, COOH, C(=0)R2e, Cl.c6 alkyl, c2_c6 alkenyl, C2_C6 alkynyl, CVC8 cycloalkyl, Ci- a C6 alkoxy group, a (Ci-C6 alkyl)amino group, a di(Ci-C6 alkyl)amino group, wherein the carbon atom in the aliphatic group of the above group may have 1, 2 or 3 Any combination of groups independently selected from the group consisting of: i, cyano, nitro, hydroxy, amine, carboxyl, CVC 6 alkyl, CVC6 alkoxy, c2_c6 alkenyloxy, C2 & block 115703.doc -29- 200806642 oxy, (VC6 haloalkoxy, and wherein R2 is selected from hydrogen, Ci_c6^, C2 -C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, (^(:6 alkoxy, (CrC6 alkyl)amine, bis(Ci-C6 alkyl)amine, phenyl and It is a heteroaryl group containing 1, 2, 3 or 4 monocyclic or bicyclic 5 to 10 membered heteroaryl rings selected from hetero atoms of 0, s and N. More specifically, the formula 1^--gas group- or tetrahydronaphthyl-amino-salina compound' wherein r is selected from the group consisting of halogen, C^_c6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, Ci-C6 alkoxy or CrC: 8 cycloalkyl, wherein the groups may be unsubstituted, partially or fully dentated. A hydrogen radical or tetrahydronaphthyl-amino-phosphonium compound of formula I wherein hydrazine is 3 and R is substituted at positions A, C and D. A dihydroindenyl or tetrahydronaphthyl-amino-oxazoline compound of the formula I wherein the melon is 2 and R2 is substituted at positions A and C. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula I wherein the melon is 2 and R2 is substituted at positions C and D. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula I wherein (f) is 1 and R2 is substituted at position A. A dihydroindenyl or tetrahydronaphthyl-amino-indenyl compound of formula I wherein the melon is 1 and R2 is substituted at position C. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazolidine compound of the formula I wherein X is S or 0. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazolidine compound of the formula I, wherein X is a dihydro-succinyl-amino-oxazoline compound of the formula I wherein S is preferably η is 1. 115703.doc -30- 200806642 Compounds of the invention can be prepared, for example, from the corresponding amine II by the synthetic route outlined in the following scheme:

la, n=n=或 x:x:o a-b-一一 ΙΙΙΞΧ 根據流程中所概括之方法，胺ιι藉由習知方式，例如藉 由使II與硫光氣反應而轉化成相應異硫氰酸鹽IV(見（例如）La, n=n= or x:x:o ab-一一 According to the method outlined in the scheme, the amine is converted to the corresponding isothiocyanate by a conventional means, for example, by reacting II with sulfur phosgene. Acid salt IV (see (for example)

Houben_Weyl, E4, ,’Methoden der Organischen Chemie”，第 lie早’第 837-842 頁，Georg Thieme Verlag 1983)。隨後， 使異硫氰酸鹽IV與胺基乙醇反應，進而獲得硫脲V。 胺基乙醇與異硫氰酸鹽以之反應可根據有機化學之標準 方法來製備’見（例如）Bi〇sci· Biotech· Biochem· 56 (7) 1062-65 (1992) 〇 因此，所獲得之硫脲V可藉由習知方式來環化，進而獲 付所要之式IIIa，b-S之嗟嗤琳化合物。化合物v之環化可在 115703.doc -31 - 200806642 因此，所獲得之硫脲v可藉由習知方式來環化，進而獲 知所要之式IIIa，b-S之嗟唾琳化合物。化合物v之環化可在 (例如）酸催化下或在脫水條件下，例如藉由光延反應 (Mitsunobu，s reaction)(見 Tetrahedron Letters 1999，4〇, 3 125-3128)來達成。 在吾人同時申報之平行美國臨時申請案中，描述該等替 代性方法。 根據流程中所概括之方法，胺Η亦可（例如）如Bi〇〇rg.Houben_Weyl, E4, , 'Methoden der Organischen Chemie', lie early 'pp. 837-842, Georg Thieme Verlag 1983). Subsequently, isothiocyanate IV is reacted with aminoethanol to obtain thiourea V. The reaction of the base ethanol with the isothiocyanate can be carried out according to standard methods of organic chemistry 'see, for example, Bi〇sci· Biotech·Biochem· 56 (7) 1062-65 (1992) 〇 Therefore, the obtained sulfur Urea V can be cyclized by a conventional means to obtain the desired compound of formula IIIa, bS. The cyclization of compound v can be found in 115703.doc -31 - 200806642. Therefore, the obtained thiourea v can be obtained. Cyclization is carried out by a conventional means to obtain the desired compound of formula IIIa, bS. The cyclization of compound v can be carried out, for example, under acid catalysis or under dehydrating conditions, for example, by a light delay reaction (Mitsunobu, s reaction) (see Tetrahedron Letters 1999, 4〇, 3 125-3128). This alternative method is described in the parallel US interim application filed by us. According to the method outlined in the process, the amine is also Can (for example) such as Bi〇〇rg.

Med. Chem· Lett. 1994, 4, 2317-22 中所述，藉由與2_ 氣乙 基異硫氰酸酯或2-氯乙基異氰酸酯之反應而轉化成唑琳 III-X且隨後在驗存在或不存在下或在下文所述之條件下來 環化。 胺II為市售的或此項技術中已知的或可藉由有機化學家 所熟悉及此項技術中熟知之方法，例如EP 2812578(二氫 茚基型胺）或US 3 95 3 5 06(四氫萘基型胺）來製備。 1-氯-2_異硫氰基乙院（CAS-登記號：6099-88-3)及2-氣乙 基異氰酸酯（CAS-登記號：1943-83-5)為市售的。 通式VI或VII之化合物可如以下流程中所概括，藉由與 (例如）如WO 2005063724中所述之烷基化劑或醯化劑之適 合親電子劑之反應來獲得。Med. Chem. Lett. 1994, 4, 2317-22, converted to oxazoline III-X by reaction with 2_ gaseous ethyl isothiocyanate or 2-chloroethyl isocyanate and subsequently tested Cyclization is carried out in the presence or absence or under the conditions described below. Amine II is commercially available or known in the art or by methods well known to organic chemists and well known in the art, such as EP 2812578 (indanylamine) or US 3 95 3 5 06 (tetrahydronaphthylamine) is prepared. 1-Chloro-2-isothiocyanatoline (CAS-Accession No.: 6099-88-3) and 2-air-ethylisocyanate (CAS-Accession No.: 1943-83-5) are commercially available. The compound of formula VI or VII can be obtained by reaction with a suitable electrophile such as an alkylating or deuterating agent as described in WO 2005063724, as outlined in the following scheme.

115703.doc •32- 200806642 特定反應混合物係通常藉由習知方 ^ A 无來處理，例如蕤占 移除溶劑、將殘餘物分配於水與適合有機溶劑之混合: 且自有機相分離產物來處理。 二氫茚基·或四氫萘基.胺基·輕化合物ι可在製備中作 為異構體混合物而獲得，然:而，若須要，則該等異構體視 合物可藉由習知方法分離成純異構體，例如藉由結晶或層 析（若必要，經光學活性吸附質）來分離。純光學活性異ς 體可（例如）自相應光學活性起始物質來合成。 一般而言，式I之二氫茚基·或四氫萘基_胺基_唑啉化合 物可藉由上文所述之方法來製備。然而，在個別狀況下， 某些化合物I亦可有利地藉由如酯水解、醯胺化、酯化、 醚裂解、烯化、還原、氧化等之其他習知方法，自其他化 合物來製備。 本發明之式I化合物之較佳實例表示於下文中： 1·式 Ι-Α 在式I化合物中，較佳者為以下式I-Α之化合物，其中 n=l、1^=11 而 X為 S :115703.doc •32- 200806642 The specific reaction mixture is usually treated by conventional methods, such as removing the solvent, distributing the residue to a mixture of water and a suitable organic solvent: and separating the product from the organic phase. deal with. Dihydroindenyl or tetrahydronaphthyl. Amine·light compound ι can be obtained as a mixture of isomers in the preparation, but: if desired, such isomers can be known by conventional means. The method is separated into pure isomers, for example by crystallization or chromatography (optionally via optically active adsorbate). Pure optically active isoindoles can be synthesized, for example, from the corresponding optically active starting materials. In general, the dihydroindenyl or tetrahydronaphthyl-amino-oxazoline compounds of formula I can be prepared by the methods described above. However, in certain instances, certain compounds I may also be advantageously prepared from other compounds by other conventional methods such as ester hydrolysis, amide amination, esterification, ether cleavage, olefination, reduction, oxidation, and the like. Preferred examples of the compound of the formula I of the present invention are shown below: 1. In the formula I, preferred are compounds of the following formula I-oxime, wherein n = 1, 1^ = 11 and X For S:

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表A之各列中所給出之含義的彼等者 115703.doc -33- 200806642 (化合物 Ι-Α·1 至 I-A.72)。 表A : iRim R2之位置： A B c D 化合物I-A.1 ch3 - - - 化合物I-A.2 - ch3 - - 化合物I-A.3 _ - ch3 - 化合物I-A.4 - - - ch3 化合物I-A.5 ch3 - ch3 - 化合物I-A.6 ch3 - ch3 ch3 化合物I-A.7 - - ch3 ch3 化合物I-A.8 Cl - - - 化合物I-A.9 Cl - 化合物I-A.10 - - Cl - 化合物I-A.ll - 麵 - Cl 化合物I-A.12 Cl - Cl - 化合物I-A.13 Cl - Cl Cl 化合物I-A.14 - - Cl Cl 化合物I-A.15 F - - - 化合物I-A.16 - F - - 化合物I-A.17 - - F - 化合物I-A.18 - - - F 化合物I-A.19 F 一 F 化合物I-A.20 F - F F 化合物I-A.21 - - F F 化合物I-A.22 Br - - - 化合物I-A.23 - Br - - 化合物I-A.24 - - Br - 化合物I_A.25 - - - Br 化合物I-A.26 Br - Br - 化合物I-A.27 Br - Br Br 化合物I-A.28 - - Br Br 化合物I-A.29 cf3 - - - 化合物I-A.30 - cf3 - - 化合物I-A.31 - - cf3 - 化合物I-A.32 cf3 化合物I-A.33 cf3 - cf3 - 化合物I-A.34 cf3 - cf3 cf3 化合物I-A.35 - 一 cf3 cf3 115703.doc -34- 200806642 TR'lm R2之位置： A B C D 化合物I-A.36 〇CF3 - - - 化合物I-A.37 - 〇CF3 - - 化合物I-A.38 - OCF3 - 化合物I-A.39 - - - 〇CF3 化合物I-A.40 OCF3 - 〇CF3 - 化合物I-A.41 OCF3 - 〇CF3 OCF3 化合物I-A.42 - - 〇CF3 OCF3 化合物I-A.43 ch3 - Cl - 化合物I-A.44 Cl ch3 - 化合物I-A.45 ch3 - F - 化合物I-A.46 F - ch3 一 化合物I-A.47 ch3 - Br 化合物I-A.48 Br - ch3 - 化合物I-A.49 ch3 - cf3 - 化合物I-A.50 cf3 - ch3 化合物I-A.51 ch3 - 〇CF3 - 化合物I-A.52 〇CF3 - ch3 - 化合物I-A.53 Cl - F - 化合物I-A.54 F - Cl - 化合物I-A.55 Cl - Br - 化合物I-A.56 Br - Cl 化合物I-A.57 Cl - cf3 - 化合物I-A.58 cf3 - Cl - 化合物I-A.59 Cl - OCF3 - 化合物I_A.60 0CF3 - Cl - 化合物I-A.61 F - Br - 化合物I-A.62 Br - F - 化合物I-A.63 F - cf3 - 化合物I-A.64 cf3 - F - 化合物I-A.65 F - 〇CF3 - 化合物I-A.66 OCF3 - F - 化合物I-A.67 Br - cf3 - 化合物I-A.68 cf3 - Br - 化合物I-A.69 Br - 〇CF3 - 化合物I-A.70 〇CF3 - Br - 化合物I-A.71 cf3 - OCF3 - 化合物I-A.72 〇CF3 - cf3 - 2.式 I-B 在式I化合物中，較佳者為以下式I-B之化合物，且其中 115703.doc -35- 200806642 n=l、R1=H且X=0，且其中變數m及R2具有下文所給出之 含義。Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table A. 115703.doc -33-200806642 (compounds Ι-Α·1 to I-A.72). Table A: Location of iRim R2: AB c D Compound IA.1 ch3 - - - Compound IA.2 - ch3 - - Compound IA.3 _ - ch3 - Compound IA.4 - - - ch3 Compound IA.5 ch3 - ch3 - Compound IA.6 ch3 - ch3 ch3 Compound IA.7 - - ch3 ch3 Compound IA.8 Cl - - - Compound IA.9 Cl - Compound IA.10 - - Cl - Compound IA.ll - Face-Cl Compound IA. 12 Cl - Cl - Compound IA.13 Cl - Cl Cl Compound IA.14 - - Cl Cl Compound IA.15 F - - - Compound IA.16 - F - - Compound IA.17 - - F - Compound IA.18 - - - F Compound IA.19 F-F Compound IA.20 F - FF Compound IA.21 - - FF Compound IA.22 Br - - - Compound IA.23 - Br - - Compound IA.24 - - Br - Compound I_A .25 - - - Br Compound IA.26 Br - Br - Compound IA.27 Br - Br Br Compound IA.28 - - Br Br Compound IA.29 cf3 - - - Compound IA.30 - cf3 - - Compound IA.31 - - cf3 - Compound IA.32 cf3 Compound IA.33 cf3 - cf3 - Compound IA.34 cf3 - cf3 cf3 Compound IA.35 - One cf3 cf3 115703.doc -34- 200806642 TR'lm Position of R2: ABCD Compound IA.36 〇CF3 - - - Compound IA.37 - 〇CF3 - - Compound IA.38 - OCF3 - Compound IA.39 - - - 〇CF3 Compound IA.40 OCF3 - 〇CF3 - Compound IA .41 OCF3 - 〇CF3 OCF3 Compound IA.42 - - 〇CF3 OCF3 Compound IA.43 ch3 - Cl - Compound IA.44 Cl ch3 - Compound IA.45 ch3 - F - Compound IA.46 F - ch3 A compound IA. 47 ch3 - Br compound IA.48 Br - ch3 - compound IA.49 ch3 - cf3 - compound IA.50 cf3 - ch3 compound IA.51 ch3 - 〇CF3 - compound IA.52 〇CF3 - ch3 - compound IA.53 Cl - F - Compound IA.54 F - Cl - Compound IA.55 Cl - Br - Compound IA.56 Br - Cl Compound IA.57 Cl - cf3 - Compound IA.58 cf3 - Cl - Compound IA.59 Cl - OCF3 - Compound I_A.60 0CF3 - Cl - Compound IA.61 F - Br - Compound IA.62 Br - F - Compound IA.63 F - cf3 - Compound IA.64 cf3 - F - Compound IA.65 F - 〇CF3 - Compound IA.66 OCF3 - F - Compound IA.67 Br - cf3 - Compound IA.68 cf3 - Br - Compound IA.69 Br - 〇CF3 - Compound IA.70 〇CF3 - Br - Compound IA.71 cf3 - OCF3 - Compound IA.72 〇CF3 - cf3 - 2. Formula IB In the compound of formula I, preferred is a compound of the following formula IB, and wherein 115703. Doc -35- 200806642 n=l, R1=H and X=0, and wherein the variables m and R2 have the meanings given below.

該等化合物之實例為其中[R2]m具有表B之各列中所給出 之含義的彼等者（化合物I-B.1至I-B.72)。 表B : [Rim R2之位置： A B C D 化合物I-B.1 ch3 - - - 化合物I-B.2 - ch3 讎 - 化合物I-B.3 - - ch3 - 化合物I-B.4 - - ch3 化合物I-B.5 ch3 - ch3 - 化合物I-B.6 ch3 - ch3 ch3 化合物I-B.7 - - ch3 ch3 化合物I_B.8 Cl - - 化合物I-B.9 - Cl - - 化合物I-B.10 - 哪 Cl - 化合物I-B.ll - - Cl 化合物I-B.12 Cl - Cl - 化合物I-B.13 Cl - Cl Cl 化合物I-B.14 - - Cl Cl 化合物I_B.15 F - - 化合物I-B.16 - F - - 化合物I-B.17 - - F - 化合物I_B.18 - - - F 化合物I-B.19 F - F - 化合物I-B.20 F 画 F F 化合物I-B.21 - - F F 化合物I-B.22 Br - - - 化合物I-B.23 - Br - - 115703.doc -36- 200806642 ϊ^ϊη R2之位置： A B c D 化合物I-B.24 - - Br - 化合物I-B.25 - - - Br 化合物I-B.26 Br - Br - 化合物I-B.27 Br - Br Br 化合物I-B.28 - - Br Br 化合物I_B.29 cf3 睡 - - 化合物I-B.30 - cf3 - - 化合物I-B.31 - - cf3 - 化合物I-B.32 - - 賺 cf3 化合物I-B.33 cf3 - cf3 - 化合物I-B.34 cf3 - cf3 cf3 化合物I-B.35 - - cf3 cf3 化合物I-B.36 OCF3 化合物I-B.37 - OCF3 - - 化合物I-B.38 - - OCF3 - 化合物I-B.39 - 麵 OCF3 化合物I-B.40 OCF3 - 〇cf3 - 化合物I-B.41 OCF3 - ocf3 OCF3 化合物I-B.42 - - OCF3 OCF3 化合物I-B.43 ch3 - Cl - 化合物I-B.44 Cl ch3 - 化合物I-B.45 ch3 - F 麵 化合物I-B.46 F - ch3 - 化合物I-B.47 ch3 - Br - 化合物I-B.48 Br - ch3 - 化合物I-B.49 ch3 - cf3 - 化合物I-B.50 cf3 - ch3 麵 化合物I-B.51 ch3 - OCF3 - 化合物I-B.52 〇CF3 - ch3 麵 化合物I-B.53 Cl - F 一 化合物I-B.54 F - Cl - 化合物I-B.55 Cl - Br - 化合物I-B.56 Br - Cl - 化合物I-B.57 Cl - cf3 - 化合物I-B.58 cf3 - Cl - 化合物I-B.59 Cl OCF3 化合物I-B.60 OCF3 - Cl - 化合物I-B.61 F - Br - 化合物I-B.62 Br - F - 化合物I-B.63 F - cf3 - 化合物I-B.64 cf3 - F - 115703.doc -37- 200806642Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table B (Compounds I-B.1 to I-B.72). Table B: [Rim R2 position: ABCD compound IB.1 ch3 - - - Compound IB.2 - ch3 雠- Compound IB.3 - - ch3 - Compound IB.4 - - ch3 Compound IB.5 ch3 - ch3 - Compound IB.6 ch3 - ch3 ch3 compound IB.7 - - ch3 ch3 compound I_B.8 Cl - - compound IB.9 - Cl - - compound IB.10 - which Cl - compound IB.ll - - Cl compound IB.12 Cl - Cl - Compound IB.13 Cl - Cl Cl Compound IB.14 - - Cl Cl Compound I_B.15 F - - Compound IB.16 - F - - Compound IB.17 - - F - Compound I_B.18 - - - F Compound IB.19 F - F - Compound IB.20 F FF Compound IB.21 - - FF Compound IB.22 Br - - - Compound IB.23 - Br - - 115703.doc -36- 200806642 ϊ^ϊη R2 Position: AB c D Compound IB.24 - - Br - Compound IB.25 - - - Br Compound IB.26 Br - Br - Compound IB.27 Br - Br Br Compound IB.28 - - Br Br Compound I_B.29 cf3 Sleep - - Compound IB.30 - cf3 - - Compound IB.31 - - cf3 - Compound IB.32 - - Earn cf3 Compound IB.33 cf3 - cf3 - Compound IB.34 cf3 - cf3 c F3 Compound IB.35 - - cf3 cf3 Compound IB.36 OCF3 Compound IB.37 - OCF3 - - Compound IB.38 - - OCF3 - Compound IB.39 - Face OCF3 Compound IB.40 OCF3 - 〇cf3 - Compound IB.41 OCF3 - ocf3 OCF3 Compound IB.42 - - OCF3 OCF3 Compound IB.43 ch3 - Cl - Compound IB.44 Cl ch3 - Compound IB.45 ch3 - F Compound IB.46 F - ch3 - Compound IB.47 ch3 - Br - Compound IB.48 Br - ch3 - Compound IB.49 ch3 - cf3 - Compound IB.50 cf3 - ch3 Compound IB.51 ch3 - OCF3 - Compound IB.52 〇CF3 - ch3 Compound IB.53 Cl - F Compound IB.54 F - Cl - Compound IB.55 Cl - Br - Compound IB.56 Br - Cl - Compound IB.57 Cl - cf3 - Compound IB.58 cf3 - Cl - Compound IB.59 Cl OCF3 Compound IB.60 OCF3 - Cl - Compound IB.61 F - Br - Compound IB.62 Br - F - Compound IB.63 F - cf3 - Compound IB.64 cf3 - F - 115703.doc -37- 200806642

以下式Ι-C之化合物 中變數m及R2具有下 ’其中 文所给 在式i化合物中，較佳者為 n=l、R^H 且 X=N-CH3，且其 出之含義。In the compound of the formula C-C, the variables m and R2 have the lower ones. Among the compounds of the formula i, preferred are n=l, R^H and X=N-CH3, and the meanings thereof.

A (I-C) 該等化合物之實例為其中[R2]m具有表c之 q 丫所給Φ 之含義的彼專者（化合物I_C」至I-C.72)。 表C :A (I-C) Examples of such compounds are those in which [R2]m has the meaning of Φ given by q in Table c (Compounds I_C" to I-C.72). Table C:

115703.doc -38 - 200806642 『Rim R2之位置： A B c D 化合物I-C.10 - - Cl - 化合物I-C.ll - - - Cl 化合物I-C.12 Cl - Cl - 化合物I-C.13 Cl - Cl Cl 化合物I-C.14 - - Cl Cl 化合物I-C.15 F - - - 化合物I-C.16 - F - - 化合物I-C.17 - - F - 化合物I-C.18 - - - F 化合物I-C.19 F - F - 化合物I-C.20 F - F F 化合物I-C.21 - F F 化合物I-C.22 Br - - - 化合物I-C.23 - Br - - 化合物I-C.24 - - Br - 化合物I-C.25 - - - Br 化合物I-C.26 Br - Br - 化合物I-C.27 Br - Br Br 化合物I-C.28 - - Br Br 化合物I-C.29 cf3 - - - 化合物I-C.30 - cf3 - - 化合物I-C.31 - - cf3 - 化合物I-C.32 - - - cf3 化合物I-C.33 cf3 - cf3 - 化合物I-C.34 cf3 - cf3 cf3 化合物I-C.35 - cf3 cf3 化合物I-C.36 OCF3 - - 化合物I-C.37 - 〇CF3 - - 化合物I-C.38 - - OCF3 - 化合物I-C.39 - - - OCF3 化合物I-C.40 OCF3 - OCF3 - 化合物I-C.41 OCF3 OCF3 OCF3 化合物I-C.42 - - OCF3 OCF3 化合物I-C.43 ch3 - Cl - 化合物I-C.44 Cl ch3 - 化合物I-C.45 ch3 F - 化合物I-C.46 F - ch3 - 化合物I_C.47 ch3 - Br - 化合物I-C.48 Br - ch3 - 化合物I-C.49 ch3 - cf3 - 化合物I-C.50 cf3 - ch3 - 115703.doc -39- 200806642 [Rim R2之位置： A B C D 化合物I-C.51 ch3 - 〇CF3 - 化合物I-C.52 OCF3 - ch3 - 化合物I-C.53 Cl - F - 化合物I-C.54 F - Cl - 化合物I-C.55 Cl - Br - 化合物I-C.56 Br - Cl - 化合物I-C.57 Cl - cf3 - 化合物I-C.58 cf3 - Cl - 化合物I-C.59 Cl - OCF3 - 化合物I-C.60 0CF3 - Cl - 化合物I-C.61 F - Br - 化合物I-C.62 Br - F - 化合物I-C.63 F cf3 - 化合物I-C.64 cf3 - F - 化合物I-C.65 F - OCF3 - 化合物I-C.66 OCF3 - F - 化合物I-C.67 Br - cf3 - 化合物I-C.68 cf3 - Br - 化合物I-C.69 Br _ 〇CF3 - 化合物I-C.70 OCF3 Br 雨 化合物I_C.71 cf3 - OCF3 - 化合物I-C.72 OCF3 - cf3 -115703.doc -38 - 200806642 "Rim R2 position: AB c D compound IC.10 - - Cl - compound IC.ll - - - Cl compound IC.12 Cl - Cl - compound IC.13 Cl - Cl Cl compound IC .14 - - Cl Cl Compound IC.15 F - - - Compound IC.16 - F - - Compound IC.17 - - F - Compound IC.18 - - - F Compound IC.19 F - F - Compound IC.20 F - FF Compound IC.21 - FF Compound IC.22 Br - - - Compound IC.23 - Br - - Compound IC.24 - - Br - Compound IC.25 - - - Br Compound IC.26 Br - Br - Compound IC.27 Br - Br Br Compound IC.28 - - Br Br Compound IC.29 cf3 - - - Compound IC.30 - cf3 - - Compound IC.31 - - cf3 - Compound IC.32 - - - cf3 Compound IC. 33 cf3 - cf3 - Compound IC.34 cf3 - cf3 cf3 Compound IC.35 - cf3 cf3 Compound IC.36 OCF3 - - Compound IC.37 - 〇CF3 - - Compound IC.38 - - OCF3 - Compound IC.39 - - - OCF3 Compound IC.40 OCF3 - OCF3 - Compound IC.41 OCF3 OCF3 OCF3 Compound IC.42 - - OCF3 OCF3 Compound IC.43 ch3 - Cl - Compound IC.44 Cl ch3 - Compound IC.45 ch3 F - Compound IC.46 F - ch3 - Compound I_C.47 ch3 - Br - Compound IC.48 Br - ch3 - Compound IC.49 ch3 - cf3 - Compound IC.50 cf3 - ch3 - 115703.doc -39- 200806642 [Rim R2 position: ABCD compound IC.51 ch3 - 〇CF3 - compound IC.52 OCF3 - ch3 - compound IC.53 Cl - F - compound IC.54 F - Cl - compound IC. 55 Cl - Br - Compound IC.56 Br - Cl - Compound IC.57 Cl - cf3 - Compound IC.58 cf3 - Cl - Compound IC.59 Cl - OCF3 - Compound IC.60 0CF3 - Cl - Compound IC.61 F - Br - Compound IC.62 Br - F - Compound IC.63 F cf3 - Compound IC.64 cf3 - F - Compound IC.65 F - OCF3 - Compound IC.66 OCF3 - F - Compound IC.67 Br - cf3 - Compound IC.68 cf3 - Br - Compound IC.69 Br _ 〇CF3 - Compound IC.70 OCF3 Br Rain Compound I_C.71 cf3 - OCF3 - Compound IC.72 OCF3 - cf3 -

4.式 I-D 在式I化合物中，較佳者為以下式I-D之化合物，其中 η=2、Ι^=Η 且 X=S :4. Formula I-D Among the compounds of formula I, preferred are compounds of formula I-D below, wherein η = 2, Ι^ = 且 and X = S:

其中變數m及R2具有下文所給出之含義。 該等化合物之實例為其中[R2]m具有表D之各列中所給出 之含義的彼等者（化合物Ι-D.l至I-D.72)。 115703.doc •40- 200806642 表D : [Rim R2之位置： A B c D 化合物I-D.1 ch3 - - - 化合物I-D.2 - ch3 - - 化合物I-D.3 - - ch3 - 化合物I-D.4 - - - ch3 化合物I-D.5 ch3 - ch3 - 化合物I-D.6 ch3 - ch3 ch3 化合物I-D.7 - - ch3 ch3 化合物I-D.8 Cl - - - 化合物I-D.9 - Cl - - 化合物I-D.10 - - Cl - 化合物I-D.ll - - - Cl 化合物I-D.12 Cl - Cl - 化合物I-D.13 Cl - Cl Cl 化合物I-D.14 - - Cl Cl 化合物I-D.15 F - - - 化合物I-D.16 F - 化合物I-D.17 - - F - 化合物I-D.18 - - - F 化合物I-D.19 F - F - 化合物I-D.20 F - F F 化合物I-D.21 - - F F 化合物I-D.22 Br 一 - - 化合物I-D.23 - Br - - 化合物I-D.24 - - Br - 化合物I_D.25 - - Br 化合物I-D.26 Br - Br - 化合物I-D.27 Br - Br Br 化合物I-D.28 - - Br Br 化合物I-D.29 cf3 - - - 化合物I-D.30 - cf3 - - 化合物I-D.31 - - cf3 - 化合物I-D.32 - - cf3 化合物I-D.33 cf3 - cf3 - 化合物I-D.34 cf3 - cf3 cf3 化合物I-D.35 - - cf3 cf3 化合物I-D.36 OCF3 - - - 化合物I-D.37 - OCF3 - - 化合物I-D.38 - - 0CF3 - 115703.doc -41 - 200806642Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table D (compounds D-D.l to I-D.72). 115703.doc •40- 200806642 Table D: [Rim R2 position: AB c D Compound ID.1 ch3 - - - Compound ID.2 - ch3 - - Compound ID.3 - - ch3 - Compound ID.4 - - - Ch3 compound ID.5 ch3 - ch3 - compound ID.6 ch3 - ch3 ch3 compound ID.7 - - ch3 ch3 compound ID.8 Cl - - - compound ID.9 - Cl - - compound ID.10 - - Cl - compound ID.ll - - - Cl Compound ID.12 Cl - Cl - Compound ID.13 Cl - Cl Cl Compound ID.14 - - Cl Cl Compound ID.15 F - - - Compound ID.16 F - Compound ID.17 - - F - Compound ID.18 - - - F Compound ID.19 F - F - Compound ID.20 F - FF Compound ID.21 - - FF Compound ID.22 Br I - - Compound ID.23 - Br - - Compound ID.24 - - Br - Compound I_D.25 - - Br Compound ID.26 Br - Br - Compound ID.27 Br - Br Br Compound ID.28 - - Br Br Compound ID.29 cf3 - - - Compound ID.30 - cf3 - - Compound ID.31 - - cf3 - Compound ID.32 - - cf3 Compound ID.33 cf3 - cf3 - Compound ID.34 cf3 - cf3 cf3 Compound ID.35 - - cf3 cf3 Was I-D.36 OCF3 - - - compound I-D.37 - OCF3 - - compound I-D.38 - - 0CF3 - 115703.doc -41 - 200806642

iR"]m R2之位置： A B C D 化合物I-D.39 - - - ocf3 化合物I-D.40 〇cf3 - ocf3 - 化合物I-D.41 〇cf3 - ocf3 〇cf3 化合物I-D.42 - ocf3 ocf3 化合物I-D.43 ch3 - Cl - 化合物I-D.44 Cl ch3 - 化合物I-D.45 ch3 - F - 化合物I-D.46 F - ch3 - 化合物I-D.47 ch3 - Br - 化合物I_D.48 Br - ch3 - 化合物I-D.49 ch3 - cf3 - 化合物I-D.50 cf3 - ch3 - 化合物I-D.51 ch3 - ocf3 - 化合物I-D.52 ocf3 - ch3 - 化合物I-D.53 Cl - F - 化合物I-D.54 F - Cl - 化合物I-D.55 Cl - Br - 化合物I-D.56 Br - Cl - 化合物I-D.57 Cl 麵 cf3 - 化合物I-D.58 cf3 - Cl - 化合物I-D.59 Cl - ocf3 - 化合物I-D.60 ocf3 Cl - 化合物I-D.61 F - Br - 化合物I-D.62 Br - F - 化合物I-D.63 F - cf3 - 化合物I-D.64 cf3 - F 化合物I-D.65 F - ocf3 - 化合物I-D.66 ocf3 - F - 化合物I-D.67 Br - cf3 - 化合物I-D.68 cf3 - Br - 化合物I-D.69 Br - ocf3 - 化合物I-D.70 ocf3 一 Br - 化合物I-D.71 cf3 - ocf3 - 化合物I-D.72 〇cf3 - cf3 - 5.式 I-E 在式I化合物中，較佳者為以下式I_E之化合物，其 n=2、RkH且 X=0 : 115703.doc -42- 200806642iR"]m R2 position: ABCD Compound ID.39 - - - ocf3 Compound ID.40 〇cf3 - ocf3 - Compound ID.41 〇cf3 - ocf3 〇cf3 Compound ID.42 - ocf3 ocf3 Compound ID.43 ch3 - Cl - Compound ID.44 Cl ch3 - Compound ID.45 ch3 - F - Compound ID.46 F - ch3 - Compound ID.47 ch3 - Br - Compound I_D.48 Br - ch3 - Compound ID.49 ch3 - cf3 - Compound ID .50 cf3 - ch3 - Compound ID.51 ch3 - ocf3 - Compound ID.52 ocf3 - ch3 - Compound ID.53 Cl - F - Compound ID.54 F - Cl - Compound ID.55 Cl - Br - Compound ID.56 Br - Cl - compound ID.57 Cl face cf3 - compound ID.58 cf3 - Cl - compound ID.59 Cl - ocf3 - compound ID.60 ocf3 Cl - compound ID.61 F - Br - compound ID.62 Br - F - Compound ID.63 F - cf3 - Compound ID.64 cf3 - F Compound ID.65 F - ocf3 - Compound ID.66 ocf3 - F - Compound ID.67 Br - cf3 - Compound ID.68 cf3 - Br - Compound ID .69 Br - ocf3 - Compound ID.70 ocf3 -Br - Compound ID.71 cf3 - ocf3 - Compound ID.72 〇cf3 - Cf3 - 5. Formula I-E Among the compounds of formula I, preferred are compounds of formula I_E below, where n = 2, RkH and X = 0: 115703.doc -42 - 200806642

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表E之各列中所給出之含義的彼等者（化 合物 I-E.1 至 I-E.72)。 表E : 『圮1 m R2之位置： A B c D 化合物I_E.l ch3 - - - 化合物Ι-Ε.2 - ch3 - - 化合物Ι-Ε.3 - - ch3 - 化合物Ι-Ε.4 - - - ch3 化合物Ι-Ε.5 ch3 - ch3 - 化合物Ι-Ε.6 ch3 - ch3 ch3 化合物Ι-Ε.7 麵 - ch3 ch3 化合物Ι-Ε.8 Cl - - - 化合物Ι_Ε.9 - Cl - - 化合物Ι-Ε.10 - - Cl - 化合物I-E.ll - - Cl 化合物Ι-Ε.12 · Cl - Cl - 化合物Ι-Ε.13 Cl - Cl Cl 化合物Ι_Ε.14 - Cl Cl 化合物Ι-Ε.15 F - - - 化合物Ι-Ε.16 - F - - 化合物Ι-Ε.17 - - F - 化合物Ι-Ε.18 - - - F 化合物Ι-Ε.19 F - F - 化合物Ι-Ε.20 F - F F 化合物Ι-Ε.21 - - F F 化合物Ι-Ε.22 Br - - - 化合物Ι_Ε.23 - Br - - 化合物Ι-Ε.24 - Br - 化合物Ι-Ε.25 - - - Br 化合物Ι-Ε.26 Br - Br - 115703.doc -43 - 200806642 [R'k R2之位置： A B c D 化合物I-E.27 Br - Br Br 化合物I-E.28 - - Br Br 化合物I-E.29 cf3 - - 化合物I-E.30 - cf3 - 化合物I-E.31 - - cf3 - 化合物I-E.32 - - - cf3 化合物I-E.33 cf3 - cf3 - 化合物I-E.34 cf3 - cf3 cf3 化合物I-E.35 - cf3 cf3 化合物I-E.36 OCF3 - - - 化合物I-E.37 - 〇CF3 - - 化合物I-E.38 - - OCF3 - 化合物I-E.39 - - OCF3 化合物I-E.40 OCF3 - OCF3 - 化合物I-E.41 OCF3 - OCF3 OCF3 化合物I-E.42 - - OCF3 0CF3 化合物I-E.43 ch3 - Cl 函 化合物I-E.44 Cl ch3 - 化合物I-E.45 ch3 - F - 化合物I-E.46 F - ch3 - 化合物I-E.47 ch3 - Br - 化合物I-E.48 Br - ch3 - 化合物I-E.49 ch3 - cf3 - 化合物I-E.50 cf3 - ch3 - 化合物I-E.51 ch3 - 〇CF3 - 化合物I-E.52 〇CF3 - ch3 - 化合物I-E.53 Cl - F - 化合物I-E.54 F 麵 Cl - 化合物I-E.55 Cl - Br - 化合物I-E.56 Br - Cl - 化合物I-E.57 Cl - cf3 - 化合物I-E.58 cf3 Cl - 化合物I-E.59 Cl - OCF3 - 化合物I-E.60 OCF3 - Cl - 化合物I-E.61 F - Br - 化合物I-E.62 Br - F 化合物I-E.63 F - cf3 - 化合物I-E.64 cf3 - F - 化合物I-E.65 F - OCF3 - 化合物I-E.66 〇CF3 - F - 化合物I-E.67 Br - cf3 - 115703.doc -44- 200806642 叱] m R2之位置： A B c D 化合物I-E.68 cf3 - Br - 化合物I-E.69 Br - ocf3 - 化合物I-E.70 〇cf3 - Br 腳 化合物I-E.71 cf3 - ocf3 - 化合物I-E.72 〇cf3 - cf3 -Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table E (compounds I-E.1 to I-E.72). Table E: "圮1 m R2 position: AB c D Compound I_E.l ch3 - - - Compound Ι-Ε.2 - ch3 - - Compound Ι-Ε.3 - - ch3 - Compound Ι-Ε.4 - - - ch3 compound Ι-Ε.5 ch3 - ch3 - compound Ι-Ε.6 ch3 - ch3 ch3 compound Ι-Ε.7 face-ch3 ch3 compound Ι-Ε.8 Cl - - - compound Ι_Ε.9 - Cl - - Compound Ι-Ε.10 - - Cl - Compound IE.ll - - Cl Compound Ι-Ε.12 · Cl - Cl - Compound Ι-Ε.13 Cl - Cl Cl Compound Ι_Ε.14 - Cl Cl Compound Ι-Ε. 15 F - - - Compound Ι-Ε.16 - F - - Compound Ι-Ε.17 - - F - Compound Ι-Ε.18 - - - F Compound Ι-Ε.19 F - F - Compound Ι-Ε. 20 F - FF Compound Ι-Ε.21 - - FF Compound Ι-Ε.22 Br - - - Compound Ι_Ε.23 - Br - - Compound Ι-Ε.24 - Br - Compound Ι-Ε.25 - - - Br The compound Ι-Ε.26 Br - Br - 115703.doc -43 - 200806642 [R'k R2 position: AB c D compound IE.27 Br - Br Br compound IE.28 - - Br Br compound IE.29 cf3 - - Compound IE.30 - cf3 - Compound IE.31 - - cf3 - Compound IE.32 - - - cf3 Compound I- E.33 cf3 - cf3 - Compound IE.34 cf3 - cf3 cf3 Compound IE.35 - cf3 cf3 Compound IE.36 OCF3 - - - Compound IE.37 - 〇CF3 - - Compound IE.38 - - OCF3 - Compound IE. 39 - - OCF3 Compound IE.40 OCF3 - OCF3 - Compound IE.41 OCF3 - OCF3 OCF3 Compound IE.42 - - OCF3 0CF3 Compound IE.43 ch3 - Cl Compound IE.44 Cl ch3 - Compound IE.45 ch3 - F - Compound IE.46 F - ch3 - Compound IE.47 ch3 - Br - Compound IE.48 Br - ch3 - Compound IE.49 ch3 - cf3 - Compound IE.50 cf3 - ch3 - Compound IE.51 ch3 - 〇CF3 - Compound IE.52 〇CF3 - ch3 - Compound IE.53 Cl - F - Compound IE.54 F Surface Cl - Compound IE.55 Cl - Br - Compound IE.56 Br - Cl - Compound IE.57 Cl - cf3 - Compound IE.58 cf3 Cl - Compound IE.59 Cl - OCF3 - Compound IE.60 OCF3 - Cl - Compound IE.61 F - Br - Compound IE.62 Br - F Compound IE.63 F - cf3 - Compound IE.64 cf3 - F - Compound IE.65 F - OCF3 - Compound IE.66 〇CF3 - F - Compound IE.67 Br - cf3 - 115703.doc -44 - 200806642 叱] m R2 position: AB c D compound IE.68 cf3 - Br - compound IE.69 Br - ocf3 - compound IE.70 〇cf3 - Br foot compound IE.71 cf3 - ocf3 - compound IE.72 〇 Cf3 - cf3 -

6.式 I-F 在式I化合物中，較佳者為以下式I-F之化合物，其中 n=2、RLH且 X=N-CH3 :6. Formula I-F In the compound of formula I, preferred are compounds of formula I-F below, wherein n = 2, RLH and X = N-CH3:

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表F之各列中所給出之含義的彼等者（化 合物 Ι-F.l 至 I-F.72)。 表F : [Rim R2之位置： A B c D 化合物I-F.l ch3 - - - 化合物I-F.2 - ch3 - - 化合物I-F.3 - ch3 - 化合物I-F.4 - - - ch3 化合物I-F.5 ch3 - ch3 化合物I-F.6 ch3 - ch3 ch3 化合物I-F.7 - - ch3 ch3 化合物I-F.8 Cl - - - 化合物I_F.9 - Cl - - 化合物I-F. 10 - - Cl - 化合物I-F.l 1 - - - Cl 化合物I-F.12 Cl - Cl - 115703.doc -45- 200806642 『Rim R2之位置： A B c D 化合物I-F.13 Cl - Cl Cl 化合物I-F.14 - - Cl Cl 化合物I-F.15 F - - - 化合物I-F.16 - F - - 化合物I-F.17 - - F - 化合物I-F.18 - - - F 化合物I-F.19 F - F - 化合物I-F.20 F - F F 化合物I-F.21 - 睡 F F 化合物I-F.22 Br - - 化合物I-F.23 - Br - - 化合物I-F.24 - - Br - 化合物I-F.25 - - Br 化合物I-F.26 Br - Br - 化合物I-F.27 Br - Br Br 化合物I-F.28 - - Br Br 化合物I-F.29 cf3 - - - 化合物I-F.30 - cf3 - - 化合物I-F.31 - - cf3 麵 化合物I-F.32 - - cf3 化合物I-F.33 cf3 - cf3 - 化合物I-F.34 cf3 - cf3 cf3 化合物I-F.35 _ - cf3 cf3 化合物I-F.36 OCF3 - 讎 化合物I-F.37 畴 OCF3 - - 化合物I-F.38 - - OCF3 - 化合物I_F.39 - - - ocf3 化合物I-F.40 〇cf3 - 0CF3 - 化合物I-F.41 ocf3 - OCF3 OCF3 化合物I-F.42 - - OCF3 OCF3 化合物I-F.43 ch3 - Cl - 化合物I_F.44 Cl ch3 - 化合物I-F.45 ch3 - F - 化合物I-F.46 F - ch3 - 化合物I-F.47 ch3 - Br - 化合物I-F.48 Br - ch3 - 化合物I-F.49 ch3 - cf3 - 化合物I-F.50 cf3 - ch3 - 化合物I-F.51 ch3 - OCF3 - 化合物I-F.52 〇CF3 - ch3 - 化合物I-F.53 Cl - F - 115703.doc -46- 200806642 iRlrn R2之位置： A B C D 化合物I-F.54 F - Cl - 化合物I-F.55 Cl Br - 化合物I-F.56 Br - Cl - 化合物I-F.57 Cl - cf3 - 化合物I-F.58 cf3 - Cl - 化合物I-F.59 Cl - 0CF3 化合物I-F.60 OCF3 - Cl - 化合物I-F.61 F Br - 化合物I-F.62 Br - F - 化合物I-F.63 F - cf3 - 化合物I-F.64 cf3 - F - 化合物I-F.65 F - 〇CF3 - 化合物I-F.66 OCF3 - F - 化合物I-F.67 Br - cf3 - 化合物I-F.68 cf3 - Br - 化合物I-F.69 Br - OCF3 - 化合物I-F.70 OCF3 - Br - 化合物I-F.71 cf3 - 〇CF3 - 化合物I-F.72 〇CF3 - cf3 -Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table F (compounds Ι-F.l to I-F.72). Table F: [Rim R2 position: AB c D Compound IF.l ch3 - - - Compound IF.2 - ch3 - - Compound IF.3 - ch3 - Compound IF.4 - - - ch3 Compound IF.5 ch3 - ch3 Compound IF.6 ch3 - ch3 ch3 Compound IF.7 - - ch3 ch3 Compound IF.8 Cl - - - Compound I_F.9 - Cl - - Compound IF. 10 - - Cl - Compound IF.l 1 - - - Cl Compound IF.12 Cl - Cl - 115703.doc -45- 200806642 "Rim R2 position: AB c D compound IF.13 Cl - Cl Cl compound IF.14 - - Cl Cl compound IF.15 F - - - compound IF. 16 - F - - Compound IF.17 - - F - Compound IF.18 - - - F Compound IF.19 F - F - Compound IF.20 F - FF Compound IF.21 - Sleep FF Compound IF.22 Br - - Compound IF.23 - Br - - Compound IF.24 - - Br - Compound IF.25 - - Br Compound IF.26 Br - Br - Compound IF.27 Br - Br Br Compound IF.28 - - Br Br Compound IF. 29 cf3 - - - Compound IF.30 - cf3 - - Compound IF.31 - - cf3 face compound IF.32 - - cf3 compound IF.33 cf3 - cf3 - compound IF.34 cf3 - cf3 cf3 IF.35 _ - cf3 cf3 Compound IF.36 OCF3 - 雠 compound IF.37 domain OCF3 - - compound IF.38 - - OCF3 - compound I_F.39 - - - ocf3 compound IF.40 〇cf3 - 0CF3 - compound IF.41 ocf3 - OCF3 OCF3 Compound IF.42 - - OCF3 OCF3 Compound IF.43 ch3 - Cl - Compound I_F.44 Cl ch3 - Compound IF.45 ch3 - F - Compound IF.46 F - ch3 - Compound IF.47 Ch3 - Br - compound IF.48 Br - ch3 - compound IF.49 ch3 - cf3 - compound IF.50 cf3 - ch3 - compound IF.51 ch3 - OCF3 - compound IF.52 〇CF3 - ch3 - compound IF.53 Cl - F - 115703.doc -46- 200806642 Location of iRlrn R2: ABCD Compound IF.54 F - Cl - Compound IF.55 Cl Br - Compound IF.56 Br - Cl - Compound IF.57 Cl - cf3 - Compound IF. 58 cf3 - Cl - Compound IF.59 Cl - 0CF3 Compound IF.60 OCF3 - Cl - Compound IF.61 F Br - Compound IF.62 Br - F - Compound IF.63 F - cf3 - Compound IF.64 cf3 - F - Compound IF.65 F - 〇CF3 - Compound IF.66 OCF3 - F - Compound IF.67 Br - cf3 - Compound I -F.68 cf3 - Br - Compound I-F.69 Br - OCF3 - Compound I-F.70 OCF3 - Br - Compound I-F.71 cf3 - 〇CF3 - Compound I-F.72 〇CF3 - cf3 -

7.式 I-G 在式I化合物中，較佳者為以下式I-G之化合物，其中 n=l、RkHsC-CO且 X=S，7. Formula I-G In the compound of formula I, preferred are compounds of the following formula I-G, wherein n = 1, RkHsC-CO and X = S,

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表G之各列中所給出之含義的彼等者 (化合物 Ι-G.l 至 I-G.72)。 115703.doc -47- 200806642 表G : [Rim R2之位置： A B c D 化合物I-G.1 ch3 - - 化合物I-G.2 - ch3 - - 化合物I-G.3 - - ch3 - 化合物I-G.4 - - - ch3 化合物I-G.5 ch3 - ch3 - 化合物I-G.6 ch3 - ch3 ch3 化合物I-G.7 - - ch3 ch3 化合物I-G.8 Cl - - - 化合物I_G.9 - Cl - - 化合物I-G.10 - - Cl - 化合物I-G.ll - - - Cl 化合物I-G.12 Cl - Cl - 化合物I-G.13 Cl - Cl Cl 化合物I-G.14 - - Cl Cl 化合物I-G.15 F - - - 化合物I-G.16 - F 讎 - 化合物I-G.17 - - F - 化合物I-G.18 - - - F 化合物I-G.19 F - F - 化合物I-G.20 F - F F 化合物I-G.21 - - F F 化合物I-G.22 Br - - 化合物I-G.23 - Br - - 化合物I-G.24 - - Br - 化合物I-G.25 - - - Br 化合物I-G.26 Br - Br - 化合物I-G.27 Br - Br Br 化合物I-G.28 - - Br Br 化合物I-G.29 cf3 - - 化合物I-G.30 - cf3 - - 化合物I-G.31 - - cf3 - 化合物I-G.32 - - - cf3 化合物I-G.33 cf3 - cf3 - 化合物I-G.34 cf3 - cf3 cf3 化合物I-G.35 - - cf3 cf3 化合物I-G.36 OCF3 - - - 化合物I-G.37 - 〇CF3 - - 化合物I-G.38 - - OCF3 - 115703.doc -48 - 200806642 [Rim R2之位置： A B C D 化合物I-G.39 - - - 〇CF3 化合物I-G.40 OCF3 - OCF3 - 化合物I-G.41 OCF3 - OCF3 〇CF3 化合物I-G.42 - - OCF3 〇CF3 化合物I-G.43 ch3 - Cl - 化合物I-G.44 Cl ch3 - 化合物I-G.45 ch3 - F - 化合物I-G.46 F - ch3 - 化合物I-G.47 ch3 - Br - 化合物I-G.48 Br - ch3 - 化合物I-G.49 ch3 - cf3 - 化合物I-G.50 cf3 - ch3 - 化合物I-G.51 ch3 - OCF3 - 化合物I-G.52 〇CF3 - ch3 - 化合物I-G.53 Cl - F - 化合物I-G.54 F - Cl - 化合物I-G.55 Cl - Br - 化合物I-G.56 Br - Cl - 化合物I-G.57 Cl - cf3 - 化合物I-G.58 cf3 - Cl - 化合物I-G.59 Cl OCF3 - 化合物I-G.60 OCF3 - Cl - 化合物I-G.61 F - Br - 化合物I-G.62 Br - F - 化合物I-G.63 F - cf3 - 化合物I-G.64 cf3 - F - 化合物I-G.65 F - OCF3 - 化合物I-G.66 OCF3 F - 化合物I-G.67 Br - cf3 - 化合物I-G.68 cf3 - Br - 化合物I-G.69 Br - OCF3 - 化合物I-G.70 OCF3 - Br - 化合物I-G.71 cf3 - OCF3 - 化合物I-G.72 〇CF3 - cf3 - 8.式 Ι-ΗWherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table G (compounds Ι-G.l to I-G.72). 115703.doc -47- 200806642 Table G: [Rim R2 position: AB c D Compound IG.1 ch3 - - Compound IG.2 - ch3 - - Compound IG.3 - - ch3 - Compound IG.4 - - - ch3 Compound IG.5 ch3 - ch3 - Compound IG.6 ch3 - ch3 ch3 Compound IG.7 - - ch3 ch3 Compound IG.8 Cl - - - Compound I_G.9 - Cl - - Compound IG.10 - - Cl - Compound IG .ll - - - Cl Compound IG.12 Cl - Cl - Compound IG.13 Cl - Cl Cl Compound IG.14 - - Cl Cl Compound IG.15 F - - - Compound IG.16 - F 雠- Compound IG.17 - - F - Compound IG.18 - - - F Compound IG.19 F - F - Compound IG.20 F - FF Compound IG.21 - - FF Compound IG.22 Br - - Compound IG.23 - Br - - Compound IG.24 - - Br - compound IG.25 - - - Br compound IG.26 Br - Br - compound IG.27 Br - Br Br compound IG.28 - - Br Br compound IG.29 cf3 - - compound IG.30 - cf3 - - Compound IG.31 - - cf3 - Compound IG.32 - - - cf3 Compound IG.33 cf3 - cf3 - Compound IG.34 cf3 - cf3 cf3 Compound IG.35 - - cf3 cf3 IG.36 OCF3 - - - Compound IG.37 - 〇CF3 - - Compound IG.38 - - OCF3 - 115703.doc -48 - 200806642 [Rim R2 position: ABCD compound IG.39 - - - 〇CF3 compound IG .40 OCF3 - OCF3 - Compound IG.41 OCF3 - OCF3 〇CF3 Compound IG.42 - - OCF3 〇CF3 Compound IG.43 ch3 - Cl - Compound IG.44 Cl ch3 - Compound IG.45 ch3 - F - Compound IG. 46 F - ch3 - compound IG.47 ch3 - Br - compound IG.48 Br - ch3 - compound IG.49 ch3 - cf3 - compound IG.50 cf3 - ch3 - compound IG.51 ch3 - OCF3 - compound IG.52 〇 CF3 - ch3 - Compound IG.53 Cl - F - Compound IG.54 F - Cl - Compound IG.55 Cl - Br - Compound IG.56 Br - Cl - Compound IG.57 Cl - cf3 - Compound IG.58 cf3 - Cl - Compound IG.59 Cl OCF3 - Compound IG.60 OCF3 - Cl - Compound IG.61 F - Br - Compound IG.62 Br - F - Compound IG.63 F - cf3 - Compound IG.64 cf3 - F - Compound IG.65 F - OCF3 - compound IG.66 OCF3 F - compound IG.67 Br - cf3 - compound IG.68 cf3 - Br - compound IG. 69 Br - OCF3 - Compound I-G.70 OCF3 - Br - Compound I-G.71 cf3 - OCF3 - Compound I-G.72 〇CF3 - cf3 - 8. Formula Ι-Η

在式I化合物中，較佳者為以下式Ι-Η之化合物，其中 n=l > R1=H3CJLX=S 115703.doc -49- 200806642Among the compounds of the formula I, preferred are compounds of the formula Ι-Η, wherein n=l > R1=H3CJLX=S 115703.doc -49- 200806642

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表Η之各列中所給出之含義的彼等者 (化合物 Ι-Η.1 至 Ι-Η.72)。 表Η ·· 『Rim R2之位置： A B C D 化合物Ι-Η.1 ch3 - - - 化合物Ι-Η.2 - ch3 - - 化合物Ι-Η.3 - - ch3 - 化合物Ι-Η.4 - - - ch3 化合物Ι-Η.5 ch3 - ch3 - 化合物Ι-Η.6 ch3 ch3 ch3 化合物Ι-Η.7 - - ch3 ch3 化合物Ι-Η.8 Cl - - - 化合物Ι-Η.9 - Cl 一 - 化合物Ι-Η.10 - - Cl - 化合物I-H.ll - - - Cl 化合物Ι-Η.12 Cl - Cl - 化合物Ι-Η.13 Cl - Cl Cl 化合物Ι-Η.14 - - Cl Cl 化合物Ι-Η.15 F - - - 化合物Ι-Η.16 - F _ - 化合物Ι_Η.17 - - F - 化合物Ι-Η.18 - - - F 化合物Ι-Η.19 F - F - 化合物Ι-Η.20 F - F F 化合物Ι-Η.21 - - F F 化合物Ι-Η.22 Br - - - 化合物Ι-Η.23 - Br - - 化合物Ι-Η.24 - - Br - 化合物Ι-Η.25 - - - Br 115703.doc -50· 200806642 [R'lm R2之位置： A B c D 化合物I-H.26 Br - Br - 化合物I-H.27 Br - Br Br 化合物I-H.28 - Br Br 化合物I-H.29 cf3 - - - 化合物I-H.30 - CFs - - 化合物I-H.31 - - cf3 - 化合物I-H.32 - - - cf3 化合物I-H.33 cf3 - cf3 - 化合物I-H.34 cf3 麵 cf3 cf3 化合物I-H.35 - - cf3 cf3 化合物I-H.36 OCF3 - - - 化合物I-H.37 - 〇cf3 一 - 化合物I-H.38 - - ocf3 - 化合物I_H.39 - - - OCF3 化合物I-H.40 OCF3 - OCF3 - 化合物I-H.41 OCF3 - OCF3 OCF3 化合物I-H.42 - - OCF3 OCF3 化合物I-H.43 ch3 - Cl - 化合物I-H.44 Cl ch3 - 化合物I-H.45 ch3 - F - 化合物I-H.46 F - ch3 _ 化合物I-H.47 ch3 - Br - 化合物I-H.48 Br - ch3 - 化合物I-H.49 ch3 - cf3 - 化合物I-H.50 cf3 - ch3 - 化合物I-H.51 ch3 - OCF3 - 化合物I-H.52 OCF3 - ch3 - 化合物I-H.53 Cl - F - 化合物I-H.54 F - Cl - 化合物I-H.55 Cl - Br - 化合物I-H.56 Br - Cl - 化合物I-H.57 Cl - cf3 - 化合物I-H.58 cf3 - Cl - 化合物I-H.59 Cl - OCF3 - 化合物I-H.60 OCF3 - Cl - 化合物I-H.61 F - Br - 化合物I-H.62 Br - F - 化合物I-H.63 F - cf3 - 化合物I-H.64 cf3 - F - 化合物I-H.65 F - 〇CF3 - 化合物I-H.66 〇CF3 - F - 115703.doc -51 - 200806642 [R'lm R2之位置： A B c D 化合物I-H.67 Br - cf3 - 化合物I-H.68 cf3 - Br - 化合物I-H.69 Br - ocf3 - 化合物I-H.70 ocf3 - Br - 化合物I-H.71 cf3 - ocf3 - 化合物I-H.72 ocf3 - cf3 -Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of the formula (compounds Ι-Η.1 to Ι-Η.72). Table Η ·· "Rim R2 position: ABCD compound Ι-Η.1 ch3 - - - Compound Ι-Η.2 - ch3 - - Compound Ι-Η.3 - - ch3 - Compound Ι-Η.4 - - - Ch3 compound Ι-Η.5 ch3 - ch3 - compound Ι-Η.6 ch3 ch3 ch3 compound Ι-Η.7 - - ch3 ch3 compound Ι-Η.8 Cl - - - compound Ι-Η.9 - Cl one- Compound Ι-Η.10 - - Cl - Compound IH.ll - - - Cl Compound Ι-Η.12 Cl - Cl - Compound Ι-Η.13 Cl - Cl Cl Compound Ι-Η.14 - - Cl Cl Compound Ι -Η.15 F - - - Compound Ι-Η.16 - F _ - Compound Ι_Η.17 - - F - Compound Ι-Η.18 - - - F Compound Ι-Η.19 F - F - Compound Ι-Η .20 F - FF Compound Ι-Η.21 - - FF Compound Ι-Η.22 Br - - - Compound Ι-Η.23 - Br - - Compound Ι-Η.24 - - Br - Compound Ι-Η.25 - - - Br 115703.doc -50· 200806642 [R'lm R2 position: AB c D compound IH.26 Br - Br - compound IH.27 Br - Br Br compound IH.28 - Br Br compound IH.29 cf3 - - - Compound IH.30 - CFs - - Compound IH.31 - - cf3 - Compound IH.32 - - - cf3 Compound IH.33 cf3 - cf3 - Compound IH.34 cf3 Face cf3 cf3 Compound IH.35 - - cf3 cf3 Compound IH.36 OCF3 - - - Compound IH.37 - 〇cf3 I - Compound IH.38 - - ocf3 - Compound I_H .39 - - - OCF3 Compound IH.40 OCF3 - OCF3 - Compound IH.41 OCF3 - OCF3 OCF3 Compound IH.42 - - OCF3 OCF3 Compound IH.43 ch3 - Cl - Compound IH.44 Cl ch3 - Compound IH.45 ch3 - F - Compound IH.46 F - ch3 _ Compound IH.47 ch3 - Br - Compound IH.48 Br - ch3 - Compound IH.49 ch3 - cf3 - Compound IH.50 cf3 - ch3 - Compound IH.51 ch3 - OCF3 - Compound IH.52 OCF3 - ch3 - Compound IH.53 Cl - F - Compound IH.54 F - Cl - Compound IH.55 Cl - Br - Compound IH.56 Br - Cl - Compound IH.57 Cl - cf3 - Compound </ RTI> IH. 64 cf3 - F - Compound IH.65 F - 〇CF3 - Compound IH.66 〇CF3 - F - 115703.doc -51 - 200806642 [R'lm R2 Position: AB c D Compound IH.67 Br - cf3 - Compound IH.68 cf3 - Br - Compound IH.69 Br - ocf3 - Compound IH.70 ocf3 - Br - Compound IH.71 cf3 - ocf3 - Compound IH.72 ocf3 - cf3 -

9.式 I-I9. Formula I-I

在式I化合物中，較佳者為以下式I-Ι之化合物，其中 n=l、R1 = CN且 X=SAmong the compounds of formula I, preferred are compounds of the formula I-Ι wherein n = 1, R1 = CN and X = S

A 其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表I之各列中所給出之含義的彼等者（化 合物 I-I.1 至 I-I.72)。 表I : [RZlm R2之位置： A B c D 化合物I-I. 1 ch3 - - - 化合物I-I.2 - ch3 - 化合物I_1.3 - - ch3 - 化合物I-I.4 - - - ch3 化合物I-I.5 ch3 ch3 - 化合物I-I.6 ch3 - ch3 ch3 化合物I-I.7 - - ch3 ch3 化合物I-I.8 Cl - - - 化合物I-I.9 - Cl - - 115703.doc -52- 200806642 rR'L R2之位置： A B c D 化合物I-I.10 - - Cl - 化合物I-I.ll - - - Cl 化合物I-I.12 Cl - Cl - 化合物I-I.13 Cl - Cl Cl 化合物14.14 - - Cl Cl 化合物I-I.15 F - - - 化合物I-I.16 - F - 麵 化合物I-I.17 - - F - 化合物I-I.18 - - - F 化合物I-I.19 F - F - 化合物I-I.20 F - F F 化合物I-I.21 - - F F 化合物I-I.22 Br - - - 化合物I-I.23 - Br - - 化合物I-I.24 - Br - 化合物I-I.25 麵 - Br 化合物I-I.26 Br - Br - 化合物I-I.27 Br - Br Br 化合物I-I.28 - - Br Br 化合物I-I.29 cf3 - - - 化合物I-I.30 - cf3 - 麵 化合物I-I.31 - - cf3 - 化合物I-I.32 - - - cf3 化合物I-I.33 cf3 - cf3 - 化合物I-I.34 cf3 - cf3 cf3 化合物14.35 - - cf3 cf3 化合物I-I.36 ocf3 - - - 化合物I-I.37 - ocf3 - - 化合物I-I.38 - - ocf3 - 化合物I-I.39 - - - ocf3 化合物I-I.40 ocf3 - ocf3 - 化合物I-I.41 ocf3 - ocf3 ocf3 化合物I-I.42 - - ocf3 ocf3 化合物I-I.43 ch3 Cl - 化合物I-I.44 Cl ch3 - 化合物I-I.45 ch3 - F - 化合物I-I.46 F - ch3 - 化合物I-I.47 ch3 - Br - 化合物I-I.48 Br - ch3 - 化合物I-I.49 ch3 麵 cf3 化合物I-I.50 cf3 - ch3 一 115703.doc -53- 200806642 [R'lm R2之位置： A B c D 化合物I-I.51 ch3 - ocf3 - 化合物I-I.52 ocf3 - ch3 - 化合物I-I.53 Cl - F - 化合物I-I.54 F - Cl - 化合物I-I.55 Cl - Br - 化合物I-I.56 Br - Cl - 化合物I-I.57 Cl - cf3 - 化合物I-I.58 cf3 - Cl - 化合物I-I.59 Cl - 〇cf3 - 化合物I-I.60 ocf3 - Cl - 化合物I-I.61 F - Br - 化合物I-I.62 Br - F - 化合物M.63 F - cf3 - 化合物I-I.64 cf3 - F - 化合物I-I.65 F - 〇cf3 - 化合物I-I.66 ocf3 - F - 化合物I-I.67 Br - cf3 - 化合物M.68 cf3 - Br - 化合物I-I.69 Br - ocf3 - 化合物M.70 ocf3 - Br - 化合物I-I.71 cf3 - ocf3 - 化合物I-I.72 〇cf3 - cf3 -A wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table I (compounds I-I.1 to I-I.72). Table I: [RZlm R2 position: AB c D compound II. 1 ch3 - - - compound II.2 - ch3 - compound I_1.3 - - ch3 - compound II.4 - - - ch3 compound II.5 ch3 ch3 - Compound II.6 ch3 - ch3 ch3 Compound II.7 - - ch3 ch3 Compound II.8 Cl - - - Compound II.9 - Cl - - 115703.doc -52- 200806642 rR'L R2 position: AB c D compound II.10 - - Cl - compound II.ll - - - Cl compound II.12 Cl - Cl - compound II.13 Cl - Cl Cl compound 14.14 - - Cl Cl compound II.15 F - - - compound II.16 - F - surface compound II.17 - - F - compound II.18 - - - F compound II.19 F - F - compound II.20 F - FF compound II.21 - - FF compound II.22 Br - - - compound II.23 - Br - - compound II.24 - Br - compound II.25 face - Br compound II.26 Br - Br - compound II.27 Br - Br Br compound II.28 - - Br Br compound II.29 cf3 - - - Compound II.30 - cf3 - Face compound II.31 - - cf3 - Compound II.32 - - - cf3 Compound II.33 cf3 - cf3 - Compound II.34 cf3 - cf3 cf3 Compound 14.35 - - cf3 cf3 Compound II.36 ocf3 - - - Compound II.37 - ocf3 - - Compound II.38 - - ocf3 - Compound II.39 - - - ocf3 Compound II.40 ocf3 - ocf3 - Compound II. 41 ocf3 - ocf3 ocf3 compound II.42 - - ocf3 ocf3 compound II.43 ch3 Cl - compound II.44 Cl ch3 - compound II.45 ch3 - F - compound II.46 F - ch3 - compound II.47 ch3 - Br - Compound II.48 Br - ch3 - Compound II.49 ch3 face cf3 compound II.50 cf3 - ch3 a 115703.doc -53- 200806642 [R'lm R2 position: AB c D compound II.51 ch3 - ocf3 - Compound II.52 ocf3 - ch3 - compound II.53 Cl - F - compound II.54 F - Cl - compound II.55 Cl - Br - compound II.56 Br - Cl - compound II.57 Cl - cf3 - compound II .58 cf3 - Cl - compound II.59 Cl - 〇cf3 - compound II.60 ocf3 - Cl - compound II.61 F - Br - compound II.62 Br - F - compound M.63 F - cf3 - compound II. 64 cf3 - F - compound II.65 F - 〇cf3 - compound II.66 ocf3 - F - compound II.67 Br - cf3 - compound M.68 Cf3 - Br - compound I-I.69 Br - ocf3 - compound M.70 ocf3 - Br - compound I-I.71 cf3 - ocf3 - compound I-I.72 〇cf3 - cf3 -

10.式 I-J 在式I化合物中，較佳者為以下式I-J之化合物，其中 n=2、rLHsC-CO且 X=S :10. Formula I-J In the compound of formula I, preferred are compounds of formula I-J below, wherein n = 2, rLHsC-CO and X = S:

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表J之各列中所給出之含義的彼等者（化 115703.doc -54- 200806642 合物 Ι-J.l 至 I-J.72)。 表J : [RZlm R2之位置： A B c D 化合物I-J.1 ch3 - - - 化合物I-J.2 - ch3 - - 化合物I-J.3 - - ch3 - 化合物I-J.4 - - - ch3 化合物I-J.5 ch3 - ch3 - 化合物I-J.6 ch3 - ch3 ch3 化合物I-J.7 - - ch3 ch3 化合物I-J.8 Cl - - - 化合物I-J.9 - Cl - - 化合物I-J.10 - Cl - 化合物I-J.ll - - Cl 化合物I-J.12 Cl - Cl - 化合物I-J.13 Cl - Cl Cl 化合物I-J.14 - - Cl Cl 化合物I-J.15 F - - - 化合物I-J.16 - F - - 化合物I-J.17 - - F - 化合物I-J.18 - - - F 化合物I-J.19 F - F - 化合物I-J.20 F F F 化合物I-J.21 - - F F 化合物I-J.22 Br - - - 化合物I-J.23 - Br - - 化合物I-J.24 - - Br - 化合物I-J.25 - - - Br 化合物I-J.26 Br - Br - 化合物I-J.27 Br - Br Br 化合物I-J.28 - Br Br 化合物I-J.29 cf3 - - - 化合物I-J.30 - cf3 - - 化合物I-J.31 - - cf3 - 化合物I-J.32 - - - cf3 化合物I-J.33 cf3 _ cf3 - 化合物I-J.34 cf3 - cf3 cf3 化合物I-J.35 - - cf3 cf3 化合物I-J.36 OCF3 - - - 115703.doc -55- 200806642 [R'lm R2之位置： A B c D 化合物I-J.37 - ocf3 - - 化合物I-J.38 - - ocf3 - 化合物I-J.39 - - ocf3 化合物I-J.40 ocf3 - 〇cf3 - 化合物I-J.41 ocf3 - 〇cf3 ocf3 化合物I-J.42 - ocf3 〇cf3 化合物I-J.43 ch3 - Cl - 化合物I-J.44 Cl ch3 - 化合物I-J.45 ch3 - F - 化合物I-J.46 F - ch3 化合物I-J.47 ch3 Br - 化合物I-J.48 Br - ch3 - 化合物I-J.49 ch3 - cf3 - 化合物I-J.50 cf3 - ch3 - 化合物I-J.51 ch3 - ocf3 - 化合物I-J.52 ocf3 - ch3 - 化合物I-J.53 Cl - F - 化合物I-J.54 F - Cl - 化合物I_J.55 Cl - Br - 化合物I-J.56 Br - Cl - 化合物I-J.57 Cl - cf3 - 化合物I-J.58 cf3 - Cl - 化合物I-J.59 Cl - ocf3 - 化合物I-J.60 ocf3 - Cl - 化合物I-J.61 F - Br - 化合物I-J.62 Br - F - 化合物I-J.63 F - cf3 - 化合物I_J.64 cf3 F - 化合物I-J.65 F - ocf3 - 化合物I-J.66 ocf3 - F - 化合物I-J.67 Br - cf3 化合物I-J.68 cf3 - Br - 化合物I-J.69 Br - ocf3 - 化合物I-J.70 ocf3 - Br - 化合物I-J.71 cf3 ocf3 - 化合物I-J.72 ocf3 - cf3 - 11.式 Ι-Κ在式I化合物中，較佳者為以下式Ι-Κ之化合物，其中 115703.doc -56- 200806642 n=2 ^ R1=H3CJLX=S ：Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table J (Chem. 115703.doc-54-200806642 Ι-J.l to I-J.72). Table J: [RZlm R2 position: AB c D Compound IJ.1 ch3 - - - Compound IJ.2 - ch3 - - Compound IJ.3 - - ch3 - Compound IJ.4 - - - ch3 Compound IJ.5 ch3 - Ch3 - compound IJ.6 ch3 - ch3 ch3 compound IJ.7 - - ch3 ch3 compound IJ.8 Cl - - - compound IJ.9 - Cl - - compound IJ.10 - Cl - compound IJ.ll - - Cl compound IJ .12 Cl - Cl - Compound IJ.13 Cl - Cl Cl Compound IJ.14 - - Cl Cl Compound IJ.15 F - - - Compound IJ.16 - F - - Compound IJ.17 - - F - Compound IJ.18 - - - F Compound IJ.19 F - F - Compound IJ.20 FFF Compound IJ.21 - - FF Compound IJ.22 Br - - - Compound IJ.23 - Br - - Compound IJ.24 - - Br - Compound IJ .25 - - - Br Compound IJ.26 Br - Br - Compound IJ.27 Br - Br Br Compound IJ.28 - Br Br Compound IJ.29 cf3 - - - Compound IJ.30 - cf3 - - Compound IJ.31 - - cf3 - Compound IJ.32 - - - cf3 Compound IJ.33 cf3 _ cf3 - Compound IJ.34 cf3 - cf3 cf3 Compound IJ.35 - - cf3 cf3 Compound IJ.36 OCF3 - - - 115703. Doc -55- 200806642 [R'lm R2 position: AB c D compound IJ.37 - ocf3 - - compound IJ.38 - - ocf3 - compound IJ.39 - - ocf3 compound IJ.40 ocf3 - 〇cf3 - compound IJ .41 ocf3 - 〇cf3 ocf3 Compound IJ.42 - ocf3 〇cf3 Compound IJ.43 ch3 - Cl - Compound IJ.44 Cl ch3 - Compound IJ.45 ch3 - F - Compound IJ.46 F - ch3 Compound IJ.47 ch3 Br - Compound IJ.48 Br - ch3 - Compound IJ.49 ch3 - cf3 - Compound IJ.50 cf3 - ch3 - Compound IJ.51 ch3 - ocf3 - Compound IJ.52 ocf3 - ch3 - Compound IJ.53 Cl - F - Compound IJ.54 F - Cl - Compound I_J.55 Cl - Br - Compound IJ.56 Br - Cl - Compound IJ.57 Cl - cf3 - Compound IJ.58 cf3 - Cl - Compound IJ.59 Cl - ocf3 - Compound IJ .60 ocf3 - Cl - Compound IJ.61 F - Br - Compound IJ.62 Br - F - Compound IJ.63 F - cf3 - Compound I_J.64 cf3 F - Compound IJ.65 F - ocf3 - Compound IJ.66 ocf3 - F - Compound IJ.67 Br - cf3 Compound IJ.68 cf3 - Br - Compound IJ.69 Br - ocf3 - Compound IJ.70 ocf3 - Br - compound IJ.71 cf3 ocf3 - compound IJ.72 ocf3 - cf3 - 11. In the compound of formula I, preferred is a compound of the formula ,-Κ, wherein 115703.doc -56- 200806642 n=2 ^ R1=H3CJLX=S :

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表K之各列中所給出之含義的彼等者 (化合物 I-K.1 至 I-K.72)。 表K : [RZlm R2之位置： A B c D 化合物I-K.1 ch3 - - - 化合物I-K.2 ch3 - 化合物I-K.3 - 麵 ch3 - 化合物I-K.4 - - - ch3 化合物I-K.5 ch3 - ch3 - 化合物I-K.6 ch3 - ch3 ch3 化合物I-K.7 - - ch3 ch3 化合物I-K.8 Cl 麵 - - 化合物I-K.9 - Cl - - 化合物I-K.10 - - Cl - 化合物I-K.ll - - - Cl 化合物I-K.12 Cl - Cl - 化合物I-K.13 Cl - Cl Cl 化合物I-K.14 - - Cl Cl 化合物I-K.15 F - - - 化合物I-K.16 - F - - 化合物I-K.17 - - F - 化合物I-K.18 - - - F 化合物I-K.19 F - F - 化合物I-K.20 F - F F 化合物I_K.21 - F F 化合物Ι-Κ.22 Br - - - 115703.doc -57· 200806642 [RZlm R2之位置： A B c D 化合物I-K.23 - Br - - 化合物I-K.24 - - Br - 化合物I-K.25 - - - Br 化合物I-K.26 Br - Br - 化合物I-K.27 Br - Br Br 化合物I-K.28 - Br Br 化合物I-K.29 cf3 - - - 化合物I-K.30 - cf3 - - 化合物I-K.31 - - cf3 - 化合物I-K.32 - - - cf3 化合物I-K.33 cf3 - cf3 - 化合物I-K.34 cf3 - cf3 cf3 化合物I-K.35 - - cf3 cf3 化合物I-K.36 OCF3 - - 化合物I-K.37 - OCF3 - - 化合物I-K.38 - 0CF3 諭 化合物I-K.39 - - - ocf3 化合物I-K.40 OCF3 - OCF3 - 化合物I-K.41 OCF3 - OCF3 OCF3 化合物I-K.42 - - 0CF3 OCF3 化合物I-K.43 ch3 - Cl - 化合物I-K.44 Cl ch3 - 化合物I-K.45 ch3 - F - 化合物I-K.46 F - ch3 - 化合物I-K.47 ch3 - Br - 化合物I-K.48 Br - ch3 - 化合物I-K.49 ch3 - cf3 - 化合物I-K.50 cf3 - ch3 - 化合物I-K.51 ch3 - OCF3 - 化合物I-K.52 OCF3 - ch3 - 化合物I-K.53 Cl - F - 化合物I-K.54 F - Cl - 化合物I-K.55 Cl - Br - 化合物I-K.56 Br - Cl - 化合物I-K.57 Cl - cf3 - 化合物I-K.58 cf3 - Cl - 化合物I-K.59 Cl - OCF3 - 化合物I-K.60 OCF3 - Cl - 化合物I-K.61 F 一 Br - 化合物I-K.62 Br - F - 化合物I-K.63 F - cf3 - 115703.doc -58 - 200806642 R2之位置： A B c D 化合物I-K.64 cf3 - F - 化合物I-K.65 F - ocf3 - 化合物I-K.66 ocf3 - F - 化合物I-K.67 Br - cf3 麵 化合物I-K.68 cf3 - Br - 化合物I-K.69 Br - 〇cf3 - 化合物I-K.70 ocf3 - Br - 化合物I-K.71 cf3 - 〇cf3 睡 化合物I-K.72 ocf3 - cf3 -Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table K (Compounds I-K.1 to I-K.72). Table K: [RZlm R2 position: AB c D Compound IK.1 ch3 - - - Compound IK.2 ch3 - Compound IK.3 - Surface ch3 - Compound IK.4 - - - ch3 Compound IK.5 ch3 - ch3 - Compound IK.6 ch3 - ch3 ch3 Compound IK.7 - - ch3 ch3 Compound IK.8 Cl Surface - - Compound IK.9 - Cl - - Compound IK.10 - - Cl - Compound IK.ll - - - Cl Compound IK .12 Cl - Cl - Compound IK.13 Cl - Cl Cl Compound IK.14 - - Cl Cl Compound IK.15 F - - - Compound IK.16 - F - - Compound IK.17 - - F - Compound IK.18 - - - F Compound IK.19 F - F - Compound IK.20 F - FF Compound I_K.21 - FF Compound Ι-Κ.22 Br - - - 115703.doc -57· 200806642 [RZlm R2 Location: AB c D Compound IK.23 - Br - - Compound IK.24 - - Br - Compound IK.25 - - - Br Compound IK.26 Br - Br - Compound IK.27 Br - Br Br Compound IK.28 - Br Br Compound IK .29 cf3 - - - Compound IK.30 - cf3 - - Compound IK.31 - - cf3 - Compound IK.32 - - - cf3 Compound IK.33 cf3 - cf3 - Compound IK.34 cf3 - cf3 cf3 Compound IK.35 - - cf3 cf3 Compound IK.36 OCF3 - - Compound IK.37 - OCF3 - - Compound IK.38 - 0CF3 谕 compound IK.39 - - - ocf3 Compound IK.40 OCF3 - OCF3 - Compound IK.41 OCF3 - OCF3 OCF3 Compound IK.42 - - 0CF3 OCF3 Compound IK.43 ch3 - Cl - Compound IK.44 Cl ch3 - Compound IK.45 ch3 - F - Compound IK.46 F - ch3 - Compound IK.47 ch3 - Br - Compound IK.48 Br - ch3 - Compound IK.49 ch3 - cf3 - Compound IK.50 cf3 - ch3 - Compound IK.51 ch3 - OCF3 - Compound IK.52 OCF3 - ch3 - Compound IK.53 Cl - F - Compound IK.54 F - Cl - Compound IK.55 Cl - Br - Compound IK.56 Br - Cl - Compound IK.57 Cl - cf3 - Compound IK.58 cf3 - Cl - Compound IK.59 Cl - OCF3 - Compound IK. 60 OCF3 - Cl - Compound IK.61 F - Br - Compound IK.62 Br - F - Compound IK.63 F - cf3 - 115703.doc -58 - 200806642 Location of R2: AB c D Compound IK.64 cf3 - F - Compound IK.65 F - ocf3 - Compound IK.66 ocf3 - F - Compound IK.67 Br - cf3 Compound IK.68 Cf3 - Br - Compound I-K.69 Br - 〇cf3 - Compound I-K.70 ocf3 - Br - Compound I-K.71 cf3 - 〇cf3 Sleep Compound I-K.72 ocf3 - cf3 -

12.式 I-L 在式I化合物中，較佳者為以下式I-L之化合物，其中 n=2、R1 = CN且 X=S :12. Formula I-L In the compound of formula I, preferred are compounds of formula I-L below, wherein n = 2, R1 = CN and X = S:

其中變數m及R2具有下文所給出之含義。該等化合物之實 例為其中[R2]m具有表L之各列中所給出之含義的彼等者（化 合物 Ι-L.l 至 I-L.72)。 表L : FR2! m R2之位置： A B c D 化合物I-L. 1 ch3 - - - 化合物I-L.2 - ch3 - - 化合物I-L.3 - - CH3 - 化合物I-L.4 - - ch3 化合物I-L.5 ch3 - ch3 - 化合物I-L.6 ch3 - ch3 ch3 化合物I-L.7 - - ch3 ch3 115703.doc -59- 200806642 [R1 m R2之位置： A B c D 化合物I-L.8 Cl - - - 化合物I-L.9 - Cl - - 化合物I_L.10 - Cl 化合物I-L.ll - - - Cl 化合物I-L.12 Cl - Cl - 化合物I-L.13 Cl - Cl Cl 化合物I-L.14 - Cl Cl 化合物I-L.15 F - - - 化合物I-L.16 - F - - 化合物I-L.17 - - F - 化合物I-L.18 - - - F 化合物I-L.19 F - F - 化合物I-L.20 F F F 化合物I-L.21 - - F F 化合物I-L.22 Br - - - 化合物I-L.23 - Br - - 化合物I-L.24 - - Br - 化合物I-L.25 - - - Br 化合物I-L.26 Br - Br - 化合物I-L.27 Br - Br Br 化合物I-L.28 - - Br Br 化合物I-L.29 cf3 - - - 化合物I-L.30 睡 cf3 - - 化合物I-L.31 一 - cf3 - 化合物I-L.32 - - cf3 化合物I-L.33 cf3 - cf3 - 化合物I-L.34 cf3 - cf3 cf3 化合物I-L.35 - - cf3 cf3 化合物I-L.36 OCF3 - - - 化合物I-L.37 - OCF3 - - 化合物I-L.38 - - OCF3 化合物I-L.39 - - OCF3 化合物I-L.40 OCF3 - OCF3 - 化合物I-L.41 OCF3 OCF3 OCF3 化合物I-L.42 - - OCF3 OCF3 化合物I-L.43 ch3 Cl - 化合物I-L.44 Cl ch3 - 化合物I-L.45 ch3 - F - 化合物I-L.46 F - ch3 - 化合物I-L.47 ch3 - Br - 化合物I-L.48 Br ch3 一 115703.doc -60- 200806642 m R2之位置： A B c D 化合物I-L.49 ch3 - cf3 - 化合物I-L.50 cf3 - ch3 - 化合物I-L.51 ch3 - ocf3 化合物I-L.52 〇CF3 - ch3 - 化合物I-L.53 Cl - F 雨 化合物I-L.54 F - Cl _ 化合物I-L.55 Cl - Br - 化合物I-L.56 Br - Cl - 化合物I-L.57 Cl - cf3 - 化合物I-L.58 cf3 - Cl - 化合物I-L.59 Cl - OCF3 - 化合物I-L.60 OCF3 - Cl - 化合物I-L.61 F - Br - 化合物I-L.62 Br - F - 化合物I-L.63 F - cf3 - 化合物I-L.64 cf3 - F - 化合物I-L.65 F - 〇CF3 - 化合物I-L.66 〇CF3 - F - 化合物I-L.67 Br cf3 化合物I-L.68 cf3 - Br 化合物I-L.69 Br - OCF3 - 化合物I-L.70 〇CF3 - Br - 化合物I-L.71 cf3 - 〇CF3 - 化合物I-L.72 〇CF3 cf3 - 由於其極好的活性，式i化合物可用於控制動物害蟲， 尤其為所選之有害昆蟲、蜘蛛類及線蟲。 式I化合物及包括其之殺蟲組合物為用於控制選自昆 蟲、蜘蛛類及線蟲之動物害蟲之有效藥劑。藉由式I化合 物控制之動物害蟲包含（例如）： 來自鱗翅類（鱗翅目之昆蟲，例如小地老 虎少/?以7(9??)、黃地老虎MgMwm)、棉葉波 紋葉蛾、黎豆夜蛾 gemmaia/以）、蘋實巢蛾conjugella)、丫紋夜 115703.doc -61 - 200806642 峨（Autographa gamma)、松樹 &amp; 竣（Bupaius piniarius)、卷 葉蛾（Cacoec/α mwrk⑽α)、棉褐帶卷蛾（Capwa reticulana)、尺蠖蛾、雲杉卷葉蛾 (C/zorbicmewra /wmz/erawa)、薔薇斜條卷葉蛾 occfiieWa/b)、美洲黏蟲（Cirp/z/s 、蘋果橐蛾 (Cj^/a /?&lt;9mo 似//&lt;2)、歐洲松毛蟲（Dwdro/z’mws 尸 kz·)、瓜野 煩(Diaphania nitidalis)、巨座玉米模（jDMiraea grandiosella)、埃及金剛鑽（Ear/似/似、小玉米埃 {Elasmopalpus lignosellus)、葡萄煩蛾{Eupoecilia ambiguella) ^ ;J+| ^ {Evetria bouliana) ^ Jtb ^ (Feltia subterranea)、尺後堪（Galleria mellonella)、孥，\、 食心義（Grapholitha funebrana)、梨，i、食心氣（Grapholitha 、棉鈴蟲（/^/ζ·οί/π·*5 armz’gera)、美洲煙葉蛾 (ββ/ζ·οί/π··ϊ vz’raa似）、美洲棉鈴蟲zea)、菜模 (Hellula undalis)、大褐楚冬墁（Hibernia defoliaria)、美感 台蛾（Hyphantria 、蘋果巢蛾（办^川⑽讲㈣仏 malinellus&quot;)、西红柿蠢蛾（Keiferia lycopersicella)、鐵衫义 ^(Lambdina fiscellaria) - ^ &quot;A ^ ^{Laphygma exigua)、 咖。非潛葉蛾（kwcopiera coffeella)-旋紋潛葉蛾 (Leucoptera sciteUa)、斑點幕形潛葉蛾（Lithocolletis blancardella)、勤每聚果小卷蛾（Lobesia botrana)、黃綠條 缚（Loxostege sticticalis)、舞毒峨山·παΓ)、僧尼 毒蛾(Lymantria monacha)、窄翅潛葉蛾{Lyonetia 、天幕毛蟲所a 卜以）、甘藍夜蛾 115703.doc -62- 200806642 {Mamestra brassicae)、^{Orgyia pseudotsugata) ^ 歐洲玉米模（OWrzWa nubilalis) ' 冬夜蛾（尸⑽o/b flammea) ^ ^cl ^{Pectinophora gossypiella) ^ H &amp; iih ^ ^ (PerzWroma sawck)、圓掌舟蛾（P/m/era 、馬铃 薯塊莖蛾(Phthorimaea operculella)、橘細潛蛾 、大菜粉蝶（P/er以 、苜稽 綠夜蛾、小菜蛾（jP/izie//a 叮/(^化//(3)、 大豆夜蛾（Pmw而〆似/α /nc/i/i/⑼*y)、松梢卷葉峨 (Rhyacionia /rw*s*ir⑽α)、番蘇潛葉蛾（ScroMpa/pw/a 、麥蛾（*S7ioiroga 、葡萄長須卷葉蛾 (Sparganothis pilleriana)、草地 $b ^XSpodoptera frugiperda)、 灰翅夜蛾（*S^(9(i(9piera littoralis)、斜故夜蛾（Spodoptera &quot;iwra)、松異帶蛾、櫟綠卷葉 蛾（Torir/x 、粉紋夜蛾（TWc/zop/wha m·)及雲杉小 ^ ^ ^ {Zeiraphera canadensis) \ 甲蟲類（勒翅目（Co/ec^kra))，例如梨長吉丁（jgr/Zw s/ziwaiws)、具條叩曱（jgrioies 、黯金針蟲 {Agriotes obscurus)、馬铃集輕金氣（Amphimallus 、迪斯帕小蠹⑽、棉鈐象甲 {Anthonomus grandis) ^ ^ ib ^ Ψ {Anthonomus pomorum) ' 繞小甜菜甲蟲//似ar/s)、大松小蠢 piniperda)、天幕枯葉蛾、蠢豆象 (Bruchus rufimanus)、窥立表（Bruchus pisorum)、烏瓦象 (5rwc/2w /⑼沿）、蘋果卷葉象甲（尽、甜菜 115703.doc -63- 200806642 大龜曱、豆葉甲（Ceroioma irz/wrcWa)、 甘藍英象曱、奈皮象甲 (C^wi/zorr/zj^c/zw 7Ζ·)、甜菜莖跳曱（C/meiocnema 、煙草金針蟲（Cc^oArws vaper/Mws)、天冬負泥 ▼ (Crioceris asparagi)、長苒葉 ψ (Diabrotica longicornis)、 十二星瓜葉曱（D/a6roi/ca 72-pwnciaia)、玉米根葉甲 (Diabrotica virgifera)、墨西哥豆瓢蟲^ (Epilachna varivestis)、煙草跳甲(Epitrix hirtipennis)、梅蹲 {Eutinobothrus brasiliensis) 松樹象甲(Hylobius 、埃及苜藉象甲（//乂pera 、苜稽葉象 曱（//χρπα 、雲杉八齒小蠢（/ps ί乂pograp/zws)、具Wherein the variables m and R2 have the meanings given below. Examples of such compounds are those in which [R2]m has the meanings given in the columns of Table L (compounds L-L.l to I-L.72). Table L: Location of FR2! m R2: AB c D Compound IL. 1 ch3 - - - Compound IL.2 - ch3 - - Compound IL.3 - - CH3 - Compound IL.4 - - ch3 Compound IL.5 ch3 - Ch3 - compound IL.6 ch3 - ch3 ch3 compound IL.7 - - ch3 ch3 115703.doc -59- 200806642 [R1 m position of R2: AB c D compound IL.8 Cl - - - compound IL.9 - Cl - - Compound I_L.10 - Cl Compound IL.ll - - - Cl Compound IL.12 Cl - Cl - Compound IL.13 Cl - Cl Cl Compound IL.14 - Cl Cl Compound IL.15 F - - - Compound IL.16 - F - - Compound IL.17 - - F - Compound IL.18 - - - F Compound IL.19 F - F - Compound IL.20 FFF Compound IL.21 - - FF Compound IL.22 Br - - - Compound IL .23 - Br - - Compound IL.24 - - Br - Compound IL.25 - - - Br Compound IL.26 Br - Br - Compound IL.27 Br - Br Br Compound IL.28 - - Br Br Compound IL.29 Cf3 - - - Compound IL.30 Sleeping cf3 - - Compound IL.31 I-cf3 - Compound IL.32 - - cf3 Compound IL.33 cf3 - cf3 - Compound IL.34 cf3 - cf3 cf3 Compound IL.35 - - cf3 cf3 Compound IL.36 OCF3 - - - Compound IL.37 - OCF3 - - Compound IL.38 - - OCF3 Compound IL.39 - - OCF3 Compound IL.40 OCF3 - OCF3 - Compound IL. 41 OCF3 OCF3 OCF3 Compound IL.42 - - OCF3 OCF3 Compound IL.43 ch3 Cl - Compound IL.44 Cl ch3 - Compound IL.45 ch3 - F - Compound IL.46 F - ch3 - Compound IL.47 ch3 - Br - Compound IL.48 Br ch3 a 115703.doc -60- 200806642 m Location of R2: AB c D Compound IL.49 ch3 - cf3 - Compound IL.50 cf3 - ch3 - Compound IL.51 ch3 - ocf3 Compound IL.52 〇 CF3 - ch3 - Compound IL.53 Cl - F Rain compound IL.54 F - Cl _ Compound IL.55 Cl - Br - Compound IL.56 Br - Cl - Compound IL.57 Cl - cf3 - Compound IL.58 cf3 - Cl - Compound IL.59 Cl - OCF3 - Compound IL.60 OCF3 - Cl - Compound IL.61 F - Br - Compound IL.62 Br - F - Compound IL.63 F - cf3 - Compound IL.64 cf3 - F - Compound IL.65 F - 〇CF3 - Compound IL.66 〇CF3 - F - Compound IL.67 Br cf3 Compound IL.68 cf3 - Br compound IL.69 Br - OCF3 - compound IL.70 〇CF3 - Br - compound IL.71 cf3 - 〇CF3 - compound IL.72 〇CF3 cf3 - due to its excellent activity, the compound of formula i can be used to control animals Pests, especially selected harmful insects, spiders and nematodes. The compounds of formula I and the pesticidal compositions comprising the same are effective agents for controlling animal pests selected from the group consisting of insects, arachnids and nematodes. Animal pests controlled by the compounds of formula I include, for example: from lepidoptera (insects of the order Lepidoptera, such as Lesser Landscaping / 7 to 9 (9??), Yellow Earth Tiger MgMwm), cotton leaf moth, Mo Bean genus gemmaia / 、), 实 巢 con 703 703 703 703 703 703 703 115703.doc -61 - 200806642 峨 (Autographa gamma), pine &amp Capwa reticulana, scorpion moth, spruce leaf moth (C/zorbicmewra /wmz/erawa), scorpion moth occfiieWa/b), American armyworm (Cirp/z/s, apple) Moth (Cj^/a /?&lt;9mo//&lt;2), European pine caterpillar (Dwdro/z'mws corpse kz·), Diaphania nitidalis, jDMiraea grandiosella , Egypt Diamond (Ear / similar, small corn eager {Elasmopalpus lignosellus), grape moth {Eupoecilia ambiguella) ^; J + | ^ {Evetria bouliana) ^ Jtb ^ (Feltia subterranea), 尺后堪 (Galleria mellonella),孥, \, 食心义 (Grapholitha funebrana), pear, i, heart (Grapholitha, cotton bollworm /^/ζ·οί/π·*5 armz'gera), American tobacco leaf moth (ββ/ζ·οί/π··ϊ vz'raa), American cotton bollworm zea), vegetable mold (Hellula undalis), large Hibernia defoliaria, Hyphantria, apple moth (do Chu (10) speak (four) 仏malinellus&quot;), Keiferia lycopersicella, Lambdina fiscellaria - ^ &quot; A ^ ^{Laphygma exigua), coffee. Non-leaching moth (kwcopiera coffeella) - Leucoptera scite Ua, Lithocolletis blancardella, Lobesia botrana, Loxostege sticticalis , Gypsum 峨α·παΓ), Lymantria monacha, Narrow-winged leaf miner {Lyonetia, Canopy caterpillar a), Cabbageworm moth 115703.doc -62- 200806642 {Mamestra brassicae), ^{Orgyia pseudotsugata ^ ^ European corn mold (OWrzWa nubilalis) ' Winter night moth (corpse (10) o / b flammea) ^ ^cl ^{Pectinophora gossypiella) ^ H &amp; iih ^ ^ (PerzWroma sawck), round palm moth (P / m / era , potato tuber moth (Phthorimaea operculella), orange fine moth, large cabbage butterfly (P / er, 苜 绿 green moth, Plutella xylostella (jP / izie / / a 叮 / (^ / / (3), Soybean californica (Pmw and similar /α /nc/i/i/(9)*y), pineapple leafhopper (Rhyacionia /rw*s*ir(10)α), Pancreatic leaf miner (ScroMpa/pw/a, wheat) Moth (*S7ioiroga, Sparganothis pilleriana, grassland $b ^XSpodoptera frugiperda), Grey-winged Spodoptera (*S^(9(i(9piera) Littoralis), Spodoptera &quot;iwra, Loose Moth, Green Leaf Moth (Torir/x, Helicoverpa armigera (TWc/zop/wha m·) and Spruce Small ^ ^ ^ { Zeiraphera canadensis) \ beetles (Co/ec^kra), such as pear long giddin (jgr/Zw s/ziwaiws), scorpion scorpion (jgrioies, gold worm ({Agriotes obscurus), horse bell set) Light golden gas (Amphimallus, Despa (10), Aphidum (Anthonomus grandis) ^ ^ ib ^ Ψ {Anthonomus pomorum) ' Around small beet beetle / / like ar / s), Dasong small stupid piniperda), canopy Dead leaf moth, stupid bean elephant (Bruchus rufimanus), squint table (Bruchus pisorum), Uva elephant (5rwc/2w / (9) along), apple leaf curl weevil (exist, beet 115703.doc -63- 200806642 big turtle, beans (Ceroioma irz/wrcWa), Cabbage 英, 皮皮甲甲 (C^wi/zorr/zj^c/zw 7Ζ·), beet stem flea (C/meiocnema, tobacco golden worm (Cc^oArws) Vaper/Mws), Crioceris asparagi, Diabrotica longicornis, Twelve Stars (D/a6roi/ca 72-pwnciaia), Corn Roots (Dia) Brotica virgifera), Epilachna varivestis, Epitrix hirtipennis, Eutinobothrus brasiliensis, pine weevil (Hylobius, Egyptian scorpion (//乂pera, 苜叶叶曱) (//χρπα, spruce eight-toothed stupid (/ps 乂乂 pograp/zws), with

條負泥轰（Lema bilineata)、1 肖負泥義（Lema melanopus) ^ 馬龄薯甲蟲、甜 菜金針蟲californicus)、福良，（Lissorhoptrus oryzophilus)、玉米金針蟲、油菜露 尾，（Meligethes 此似ι/s)、忽布總角金龜 hippocastanl)、西方 1 矜魏金 HMelolontha melolonthcT)、 稻負泥義（Oulema or少zae)、槽象甲 •yw/caiws)、草莓根象甲（C^brr/zync/zws ovaiws)、芥末甲蟲 (Phaedon cochleariae)、油菜藍跳 ψ (Phyllotreta c/zrpocep/m/a)、金龜子sp·)、庭園麗金龜 (Phyllopertha horticola)、蕪菁淡足跳甲 nemorum)、黃曲條跳曱、日本麗金 說（Popillia japonica)、窥瓦葉 I，[Sitona lineatus)反數 I 115703.doc -64- 200806642 (Sitophilus grartaria) \ 雙翅類（雙翅目，例如埃及伊蚊（deda wgXP&quot;)、剌擾伊蚊（乂以以 να⑽s)、墨西哥橘實繩 (Anastrepha ludens)、M ^ ^(Anopheles maculipennis) % 地中海實绳（C^raiz’i以ca/7/ίαία)、蛆症金繩 bezziana)、美洲金繩（C/zrpomya hominivorax) ^ ^ 4¾ (Chrysomya macellaria) ^ 高梁癭虫文sorghicola)、 盾波繩、五帶淡色庫蚊（Cw/ex 、瓜實繩（_Dacw*y ewcwrMiae)、油撤揽實繩（JDaews o/eae)、芸苔莢瘦蚊（Dadnewra 、黃腹废蠅 {Fannia canicularis)、欠馬％ 纖{Gasterophilus intestinalis、、 刺舌繩（G/oaha 、騷擾角繩 irritans)、馬鞍形糖蚊叫i/eWrzi)、種繩 户/aiwra)、紋皮繩（//兄//加αία)、美洲斑 潛繩（L/r/omyza saiz’vae)、非洲菊斑潛繩（Lirz’omyza trifolii)、山羊綠题（Zwcz7z’a Mpr/⑽）、銅綠織 cuprina)、絲光綠繩[Lucilia sericata) Lycoria 、黑森麥桿繩、家绳 (Mwkq 、廄腐繩（Mwscha siMw/⑽s)、羊鼻繩 ov/s)瑞典麥稈蠅（(9%ζ·⑽//a /Hi)、甜菜潛葉蠅 {Pegomya hysocyami)、^ ^ ^ 4¾ {Phorbia antiqua) Λ ^ 草種繩（jP/zorWa brassicae)、窄草種绳（P/zorMa aardWa)、櫻桃實蠅ceras/)、蘋果實蠅 (Rhagoletis pomonella) ^ ^ it {Tabanus 、甘藍大 115703.doc •65- 200806642 故（Tipula oleracea)反歡洲大蚊（Tipula paludosa) ·， 薊馬（纓翅目，例如蘭花薊馬 (Dichromothrips 、煙草褐薊馬（Fr⑽ /wsea)、苜蓿莉馬、花萄馬 ir/i/cz·)、橘實莉馬c/irz·)、稻刻 馬、Thrips &lt;9r;；2：(3e)、南黃薊馬（77zr(ps 及煙薊馬 (Thrips tabaci)； 膜翅類（膜翅目，例如新疆菜葉蜂 rwae)、切葉蟻、南美切葉蟻 、德州切葉蟻（j/ia iex⑽α)、小長角葉蜂 ⑽ 、歐洲蘋果長角葉蜂 、蔚蟻（Mow&lt;9wor/wm 、熱帶火蟻 (Solenopsis geminata)SL ^ ^^{Solenopsis invicta)； 異翅類（異翅目，例如喜綠墙（dcrwierwz/w /n7are)、多毛長蜂（Β/ζ·μι/·5 /ewcc^ierws)、煙草黑斑盲墙 [Cyrtopeltis notatus)、梅 1工锋（Dysdercus cingulatus、、中 間椿象hierme山·ι/*9)、麥扁盾蝽（jBwrygaWer integriceps)、梅褐蜂（Euschistus impictiventris)、葉足緣蜂 /^/^//叩心）、牧草盲墙（Lj/gz/s /kec^arz\s〇、牧 草盲蝽（Z^ygws 、稻綠墙vz’r/dw/a)、甜菜 撿網墙（Ρί以、紫臭蝽（*S(9/wZ&gt;ea 及缚 KThyanta perditor) ·， 同翅類（同翅目（从⑽叩kra))， 例如驢豆财 {Acyrthosiphon onobrychis)、落葉松球财 115703.doc -66- 200806642 laricis)、1 爾场 QAphidula nasturtiV)、暮 I 所（Aphis /ake)、佛氏虫牙/br6e*yz·)、蘋果财 pomz·)、棉財 «ρ/π、、醋栗财 «ρ/π·β groMw/arz·以）、施氏财 «p/ni sc/mezWerz·)、繡線菊财、山茨財 (Aphis sambucf)、銳豆财 QAcyrthosiphon pisum)、馬铃集長 須虫牙{Aulacorthum solani)、銀葉粉風（万 emzWa argeWzyb/&quot;)、薊短尾虫牙（价ac/^c⑽cardwz·)、圓尾财 (Brachycaudus helichrysi)、桃票、短尾场（Brachycaudus persicae)、梅场 QBrachycaudus prunicofa)、甘藍財 (Brevicoryne brassicae)、魚冬j 毛场[Capitophorus hornf)、 Cerosipha gossypii 、專萬：毛管场（Chaetosiphon /rag〜/b///·)、茶蘼隱瘤額财（〇兄piomj/zws rAb)、諾曼尼椎 球財（Drey/'wha nordmannianae)、雲杉椎球财（Dr^y/ws/a piceae)、根瘤蜗 QDysaphis radicola)、Dysaulacorthum pseudosolani、蘋粉紅劣虫牙p/aniagz·似a)、梨财 (Dysaphis pyri)、蠢豆微葉缉（Empoasca fabae)、梅大尾场 (Hyalopterus pruni) 茶薦苦菜财 /aciwcw)、麥長管呀（Macrwz’p/zwm 、大戟長管财 {Macrosiphum euphorbiae)、暮藏 I 管蜗[Macrosiphon rosae)、蠢立修 I 缉（Megoura viciae)、Melanaphis pyrarius、I 薇麥蜗[Metopolophium dirhodum)、桃财 、冬蒽财（Myzws、櫻桃黑 瘤額财（均cerasz·)、Myzus persicae、變異财（Myzws 、高宜虫牙rzHn/gr/)、褐稻乱 115703.doc -67- 200806642 (Nilaparvata lugens)、嚢柄癟綿蚜（pemphigUS bursarius)、 蔗飛虱（ΡπΗ似MCc/mr/czWa)、蛇麻疣額蚜 /2wmw&quot;)、蘋木鼠〇Ρπ//α ma/z·)、梨木風（尸ρζ&gt;ζ·)、冬蔥溢瘤 场（Rhopalomyzus ascalonicus)、i ^ ^ ^ ^ {Rhopalosiphum mazWz\y)、禾穀縊管蚜pa山·）、蘋果草縊管 蜗（Rhopalosiphum insertum)、馬拉圓尾蚜（Sappap/ni mda)、馬利圓尾蚜（心即叩/π) ma/z·)、麥二叉蚜（Sc/z/zap/n) gramziwm)、裂鞘葉蚜（Sc/nioMwra /awwgz〜）、麥長管蚜 (Sitobion avenae) - (Sogatella furcifera)溫室白粉虱 {Trialeurodes vaporariorum) - A # (Toxoptera aurantiiand) 及葡萄根瘤虫牙（Ww Wi//b/z·/); 白蟻類（等翅目（Isoptera))，例如黃頸白蟻（Calotermes flavicollis)、黃足白蟻（Leucotermes flavipes)、黃胸散白蟻 (Reticulitermes flavipes)、南歐網紋白蛾（Reticulitermes lucifugus)及納塔爾白蟻（Termes natalensis); 直翅類（直翅目（Orthoptera))，例如家遞蟀（Acheta domestica)、東方蜚蠊（Blatta orientalis)、德國小蠊 (Blattella germanica)、歐洲球螋（Forficula auricularia)、歐 洲埃蛄（Gryllotalpa gryllotalpa)、飛虫皇（Locusta migratoria)、 雙帶蚱猛（Melanoplus bivittatus)、紅腿虫皇（Melanoplus femur-rubrum)、墨西哥蚱猛（Melanoplus mexicanus)、遷徙 蚱猛（Melanoplus sanguinipes)、落磯山蚱猛（Melanoplus spretus)、紅翅虫皇（Nomadacris septemfasciata)、美洲大蠊 (Periplaneta americana)、美洲虫令猛（Schistocerca americana)、 115703.doc -68- 200806642 棕尾蚱猛（Schistocerca peregrina)、摩洛哥蟲（Stauronotus maroccanus)及溫室蛾、螽（Tachycines asynamorus); 虫知蛛綱（Arachnoidea)，諸如4知蛛類（蜱蜗目（Acarina))， 例如軟蜱科（Argasidae)、蜱科（Ixodidae)及療蜗科 (Sarcoptidae)，諸如美洲花蜱（Amblyomma americanum)、 彩飾花蜱（Amblyomma variegatum)、波斯隱嗓蜱（Argas persicus)、具環方頭碑（Boophilus annulatus)、無紋牛蜱 (Boophilus decoloratus)、微小牛蜱（Boophilus microplus)、 森林革蜱（Dermacentor silvarum)、長蝝璃眼碑（Hyalomma truncatum)、羊硬蜱（Ixodes ricinus)、紅硬蜱（Ixodes rubicundus)、嗓蜱（Ornithodorus moubata)、耳殘 口彖蜱 (Otobius megnini)、雞皮刺瞒（Dermanyssus gallinae)、羊 癢蜗（Psoroptes ovis)、具尾扇頭蜱（Rhipicephalus appendiculatus)、紅腿扇頭蜱（Rhipicephalus evertsi)、济 虫茜（Sarcoptes scabiei)及諸如蘋刺瘦蜗（Aculus schlechtendali)、橘鏽蜗（Phyllocoptrata oleivora)及掛桔癭 蜗（Eriophyes sheldoni)之瘿蜗類（Eriophyidae spp·);諸如 仙客來蜗(Phytonemus pallidus)及多食跗線蟎 (Polyphagotarsonemus latus)之财線虫茜類（Tarsonemidae spp.)；諸如紫偽葉瞒（Brevipalpus phoenicis)之細須蜗類 (Tenuipalpidae spp.)；諸如朱砂葉蜗（Tetranychus cinnabarinus)、神澤氏葉蜗科（Tetranychus kanzawai)、太 平洋紅葉蜗（Tetranychus pacificus)、棉紅葉瞒（Tetranychus telarius)及棉葉蜗（Tetranychus urticae)、蘋果紅物蛛 115703.doc -69- 200806642 (Panonychus ulmi)、橘全爪蜗（Panonychus citri)及草地小 瓜蜗（Oligonychus pratensis)之葉瞒類（Tetranychidae spp·); 蚤目（siphonatera)，例如印度鼠蚤（Xenopsylla cheopis)、 角葉蚤屬（Ceratophyllus spp)。 組合物及式I化合物適用於控制線蟲，尤其為植物寄生 線蟲，諸如根結線蟲類，北方根結線蟲（Meloidogyne hapla)、南方根結線蟲（Meloidogyne incognita)、爪口圭根結 線蟲（Meloidogyne javanica)及其它根結線蟲屬 (Meloidogyne)物種；胞囊線蟲類，馬鈴薯金線蟲 (Globodera rostochiensis)及其它胞囊線蟲（Globodera)物 種；小麥胞囊線蟲（Heterodera avenae)、大豆胞囊線蟲 (Heterodera glycines)、甜菜胞囊線蟲（Heterodera schachtii)、三葉草胞囊線蟲（Heterodera trifolii)及其它胞 囊線蟲屬（Heterodera)物種；種子蟲癭線蟲類，蛇墊刃屬 (Anguina)物種；莖及葉線蟲類，滑刃線蟲屬 (Aphelenchoides)物種；螯針線蟲類，刺線蟲（Belonolaimus longicaudatus)及其它螯針線蟲（Belonolaimus)物種；松線 蟲類，松材線蟲（Bursaphelenchus xylophilus)及其它傘滑 刃屬（Bursaphelenchus)物種；環線蟲類，環線蟲屬 (Criconema)物種、環紋線蟲（Criconemella)物種、似環線 蟲屬（Criconemoides)物種、中環線蟲（Mesocriconema)物 種；莖及球線蟲，馬鈴薯腐爛莖線蟲（Ditylenchus destructor)、玉米莖線蟲（Ditylenchus dipsaci)及其它雙塾 115703.doc -70- 200806642 刃屬（Ditylenchus)物種；錐線蟲類，錐線蟲（Dolichodorus) 物種；螺旋線蟲類，香蕉螺旋形線蟲（Helicotylenchus multicinctus)及其它螺旋線蟲屬（Helicotylenchus)物種；外 鞘線蟲類及勒線蟲類，鞘線蟲（Hemicycliophora)物種及半 輪線蟲屬（Hemicriconemoides)物種；稻根線蟲 (Hirschmanniella)物種；槍線蟲類，冠線蟲（Hoplolaimus) 物種；假根結線蟲類，珍珠線蟲（Nacobbus)物種；針線蟲 類，伸長長針線蟲（Longidorus elongatus)及其它長針線蟲 屬（Longidorus)物種；釘線蟲類，擬墊刃屬（Paratylenchus) 物種；腐線蟲類，加州根腐線蟲（Pratylenchus neglectus)、北方根腐線蟲（Pratylenchus penetrans)、彎曲 根腐線蟲（Pratylenchus curvitatus)、損傷根腐線蟲 (Pratylenchus goodeyi)及其它草地墊刃線蟲屬 (Pratylenchus)物種；掘穴線蟲類，掘穴線蟲（Radopholus similis)及其它内侵線蟲屬（Radopholus)物種；腎形線蟲 類’強狀盤旋線蟲（Rotylenchus robustus)及其它盤旋線蟲 (Rotylenchus)物種；螺旋線蟲（Scutellonema)物種；殘根線 蟲類’克伯氏殘根線蟲（Trichodorus primitivus)及其它殘 根線蟲（Trichodorus)物種、擬毛刺線蟲屬（Paratrichodorus) 物種；短小線蟲類，煙草矮化線蟲（Tylenchorhynchus claytoni)、不定矮化線蟲（Tylenchorhynchus dubius)及其它 矮化線蟲（Tylenchorhynchus)物種；橘線蟲類，墊刃線蟲屬 (Tylenchulus)物種；劍線蟲類，劍線蟲（xiphinema)物種； 及其它植物寄生線蟲物種。 115703.doc 200806642 在本發明之一較佳實施例中，式i化合物適用於控制昆 蟲或：t知蛛類，尤其為鱗翅目、鞘翅目及同翅目之昆蟲及蜱 蜗目之細蛛類。根據本發明之式I化合物尤其適用於控制 鱗翅目及同翅目之昆蟲。 調配物 因此’本發明進一步提供對抗該等動物害蟲之農業組合 物’其包括該一定量之至少一種式〗化合物或至少一種I之 農業上適用鹽及具有殺蟲作用之至少一種惰性液體及/或 固體農藝學上可接受之載劑及（若須要）至少一種界面活性 劑。 該組合物可含有根據本發明之單一式I活性化合物或其 對映異構體或若干活性化合物I之混合物。根據本發明之 組合物可包括個別異構體或異構體之混合物以及個別互變 異構體或互變異構體之混合物。 為用於根據本發明之方法，化合物I可轉化成習用調配 物，例如溶液、乳液、懸浮液、微塵、粉末、糊狀物、顆 粒及可直接噴霧之溶液。使用形式視特定目的及應用方法 而定。調配物及應用方法經選擇以在各狀況下確保根據本 發明之式I化合物之精細及均一分佈。 調配物係以已知方式來製備（見（例如）評論us 3，060,084、ΕΡ·A 707 445(對液態濃縮物而言），Browning， ’’Agglomeration’’，Chemical Engineering，Dec· 4，1967，147-48，Perry’s Chemical Engineer’s Handbook，第 4 版， McGraw-Hill，New York，1963，第 8-57 頁以及下列等等： 115703.doc -72- 200806642 WO 91/13546 、US 4，172,714 、US 4，144,050、US 3,920,442、US 5，180,587、US 5,232,701、US 5,208,030、 GB 2,095,558、US 3,299,566，Klingman，Weed Control as a Science，John Wiley 及 Sons，Inc.，New York，1961， Hance 等人，Weed Control Handbook，第 8版，Blackwell Scientific Publications, Oxford， 1989 及 Mollet， H·， Grubemann, A., Formulation technology, Wiley VCH Verlag GmbH，Weinheim (Germany)，2001，2. D. A. Knowles， Chemistry and Technology of Agrochemical Formulations， Kluwer Academic Publishers，Dordrecht，1998 (ISBN 0-7514-0443·8))，例如藉由將活性化合物攙入適用於農用化 學品之調配物之助劑，諸如溶劑及/或載劑、（若須要）乳化 劑、界面活性劑及分散劑、防腐劑、消泡劑、防束劑，對 種子處理調配物而言，亦視情況攙入著色劑及/或黏合劑 及/或膠凝劑來製備。 適合之溶劑/載劑為（例如）·· 溶劑，諸如水、芳族溶劑（例如Solvesso產品、二甲苯及 其類似物）、石蠟（例如礦物餾份）、醇（例如曱醇、丁醇、 戊醇、苄醇）、_ (例如環己_、Γ- 丁内酯）、吼洛唆酮（N-甲基-吼咯啶酮（NMP)、N-辛基吡咯啶酮（NOP))、乙酸酯 (二乙酸乙二醇酯）、乳酸烷酯、諸如Γ-丁内酯之内酯、乙 二醇、脂肪酸二甲基醯胺、脂肪酸及脂肪酸酯、三甘油 酯、蔬菜或動物源油及諸如烧基化植物油之改質油。原則 上，亦可使用溶劑混合物。 115703.doc •73- 200806642 載劑，諸如經研磨之天然礦物及經研磨之合成礦物，諸 如矽膠、細粉狀矽酸、矽酸鹽、滑石粉、高嶺土、美國活 性白土、石灰石、石灰、白堊、紅玄武土、黃土、黏土、 白雲石、矽藻土、硫酸鈣及硫酸鎂、氧化鎂、經研磨之合 成材料’諸如硫酸銨、填酸銨、确酸銨、尿素之肥料及諸 如榖類粕粉、樹皮粕粉、木材粕粉及堅果殼粕粉、纖維素 粉末之植物源產品及其他固體載劑。 適合之乳化劑為非離子及陰離子乳化劑（例如聚環氧乙 烷脂肪醇醚、烷基磺酸酯及芳基磺酸酯）。 分散劑之實例為木質素亞硫酸鹽廢液及甲基纖維素。 適合之界面活性劑為木質磺酸、萘磺酸、酚磺酸、二丁 基萘磺酸之鹼金屬、鹼土金屬及銨鹽，烷基芳基磺酸酯， 烧基硫酸酯，烧基績酸酯，脂肪醇硫酸酯，脂肪酸及硫酸 化脂族醇二醇醚，此外磺化萘及萘衍生物與曱醛之縮合 物’萘與盼及甲酸之縮合物或萘石黃酸與紛及甲酸之縮合 物’聚環氧乙烷辛基苯基醚，乙氧基化異辛基酚，辛基 酚’壬基酚，烷基苯基聚乙二醇醚，三丁基苯基聚乙二醇 醚，三硬脂醯基苯基聚乙二醇醚，烷基芳基聚醚醇，醇及 脂肪醇/氧化乙烯縮合物，乙氧基化蓖麻油，聚環氧乙烷 烷基醚，乙氧基化聚氧丙烯，月桂醇聚乙二醇醚縮醛，山 梨醇酯。 又，可向調配物中添加諸如甘油、乙二醇、丙二醇之防 ;東劑及諸如殺菌劑。 適合之消泡劑為（例如）基於矽或硬脂酸鎂之消泡劑。 115703.doc -74- 200806642 適合之防腐劑為（例如）二氯酚及苄醇半甲縮醛。 適合之增稠劑為使調配物具有假塑性流動行為，亦即靜 止時為咼黏度且在攪動階段中為低黏度之化合物。在本文 中’可提及（例如）基於多醣之市售增稠劑，諸如XanthanLema bilineata, 1 Lema melanopus ^ horse-eared beetle, californicus, Fussian, Lisorhoptrus oryzophilus, golden worm, rape, tail, (Meligethes) /s), 布 角 角 hippocastanl), West 1 矜 金 HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM HM Zync/zws ovaiws), mustard beetle (Phaedon cochleariae), rapeseed blue flea (Phyllotreta c/zrpocep/m/a), chafer sp.), Phyllopertha horticola, turnip nemum, yellow Curl fleas, Popillia japonica, Sitona lineatus, I 115703.doc -64-200806642 (Sitophilus grartaria) \ Diptera (Diptera, eg Aedes aegypti ( Deda wgXP&quot;), harassing Aedes mosquitoes (乂αα(10)s), Anastrepha ludens, M^^(Anopheles maculipennis)% Mediterranean solid rope (C^raiz'i ca/7/ίαία), Sickle golden rope bezziana), American golden rope (C/zrpomya h Ominivorax) ^ ^ 43⁄4 (Chrysomya macellaria) ^ Sorghum sorghicola, Shield wave rope, Culex pipiens pallens (Cw/ex, melon rope (_Dacw*y ewcwrMiae), oil withdrawal rope (JDaews o/ Eae), Drosnewra, Fannia canicularis, Gasterophilus intestinalis, G/oaha, irritans, saddle-shaped mosquitoes i/ eWrzi), seed rope household / aiwra), leather rope (//brother / / plus αία), American spotted dive rope (L/r/omyza saiz'vae), African chrysanthemum (Lirz'omyza trifolii), Goat Green (Zwcz7z'a Mpr/(10)), copper green cuprina), Lucilia sericata Lycoria, Hessian wheat rope, home rope (Mwkq, 廄腐(Mwscha siMw/(10)s), sheep nose rope Ov/s) Swedish wheat worm ((9% ζ·(10)//a/Hi), beet leaf miner {Pegomya hysocyami), ^ ^ ^ 45⁄4 {Phorbia antiqua) Λ ^ grass seed rope (jP/zorWa brassicae) , narrow grass rope (P/zorMa aardWa), cherry fruit fly ceras /), apple fruit fly (Rhagoletis pomonella) ^ ^ it {Tabanus, cabbage big 115703.doc •65- 200806642 Therefore (Tipul a oleracea) Tipula paludosa · 蓟 缨 (缨ptera, such as orchid thrips (Dichromothrips, tobacco brown pelicans (Fr(10) /wsea), 苜蓿莉马, 萄马 ir/i/cz ·), Orange Lima c/irz·), Inscribed Horse, Thrips &lt;9r;; 2: (3e), Southern Yellow Horse (77zr (ps and Thrips tabaci); Membrane (film) Hymenoptera, such as Xinjiang leaf bee rwae, leaf-cutting ants, South American leaf-cutting ants, Texas leaf-cutting ants (j/ia iex (10) α), small long-horned bees (10), European apple long-horned bees, ants (Mow&lt; 9wor/wm, Solenopsis geminata SL ^ ^^{Solenopsis invicta); Heteroptera (Hymenoptera), such as the green wall (dcrwierwz/w /n7are), the hairy bee (Β/ζ·μι/· 5 /ewcc^ierws), Cyrtopeltis notatus, Dysdercus cingulatus, hierme mountain·ι/*9, jBwrygaWer integriceps, plum brown bee Euschistus impictiventris), leaf foot bee /^/^//叩 heart), pasture blind wall (Lj/gz/s /kec^arz\s〇, pasture blind 蝽 (Z^ygws, rice green wall vz'r/ Dw/a), beet Net wall (Ρί以, purple skunk (*S(9/wZ&gt;ea and bound KThyanta perditor) ·, the same winged species (Homoptera (from (10)叩kra)), such as 驴豆财{Acyrthosiphon onobrychis), larch ball Finance 115703.doc -66- 200806642 laricis), 1 field QAphidula nasturtiV), 暮I (Aphis /ake), worm teeth /br6e*yz·), apple money pomz·), cotton money «ρ/π, , vinegar money «ρ/π·β groMw/arz·), Shishicai «p/ni sc/mezWerz·), Spirochetes, Aphis sambucf, QAcyrthosiphon pisum) Malay episodes {Aulacorthum solani), silver leaf powder wind (wan emzWa argeWzyb/&quot;), 蓟 尾 牙 ( (price ac / ^ c (10) cardwz ·), round tail Cai (Brachycaudus helichrysi), peach ticket, short tail field ( Brachycaudus persicae), QBrachycaudus prunicofa), Brevicoryne brassicae, Capitophorus hornf, Cerosipha gossypii, tens of thousands: capillary field (Chaetosiphon /rag~/b///·), samovar隐瘤额财(〇兄piomj/zws rAb), Normany vertebrate (Drey/'wha nordmannianae), spruce vertebrate Dr^y/ws/a piceae), Rhizosphere genus QDysaphis radicola, Dysaulacorthum pseudosolani, P. aniagz, a), Dysaphis pyri, Empoasca fabae, Mei Da The end of the field (Hyalopterus pruni) tea recommended bitter food / aciwcw), wheat long tube (Macrwz'p / zwm, big 戟 long tube wealth {Macrosiphum euphorbiae), I I I tube [ [Macrosiphon rosae), stupid vertical repair I Megoura viciae, Melanaphis pyrarius, I Metopolophium dirhodum, Taocai, Dongqicai (Myzws, cherry melanoma (Cerasz), Myzus persicae, Mutant (Myzws, Gaoyi fangs rzHn) /gr/), brown rice chaos 115703.doc -67- 200806642 (Nilaparvata lugens), mph 瘪 pe (pemphigUS bursarius), cane toad (ΡπΗlike MCc/mr/czWa), python 疣 蚜 /2wmw&quot ;), Phyllostachys 〇Ρ / / / α ma / z ·), pear wood wind (corpse ζ ζ gt ) 、 、 、 、 、 、 、 、 、 、 、 、 冬 冬 冬 冬 冬 冬 冬 R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R谷缢管蚜pa山·), apple grass 缢 缢 (Rhopalosiphum insertum), Mara round 蚜 (Sappap/ni mda) , Marley round-tailed pheasant (heart is 叩 / π) ma / z ·), wheat bifurcation (Sc / z / zap / n) gramziwm), cracked sheath leaf 蚜 (Sc / nioMwra / awwgz ~), long tube S(Sitobion avenae) - (Sogatella furcifera) greenhouse whitefly Tri{Trialeurodes vaporariorum - A # (Toxoptera aurantiiand) and grape root nodule (Ww Wi//b/z·/); termites (Isoptera) For example, Calotermes flavicollis, Leucotermes flavipes, Reticulitermes flavipes, Reticulitermes lucifugus and Termes natalensis; Orthoptera (straight Orthoptera, such as Acheta domestica, Blata orientalis, Blattella germanica, Forficula auricularia, Gryllotalpa gryllotalpa, flying insects Locusta migratoria, Melanoplus bivittatus, Melanoplus femur-rubrum, Melanoplus mexicanus, Melanoplus sanguinipes, and Rocky Mountains Elanoplus spretus), Nomadacris septemfasciata, Periplaneta americana, Schistocerca americana, 115703.doc -68-200806642 Schistocerca peregrina, Moroccan worm (Stauronotus Maroccanus) and greenhouse moth, Tachycines asynamorus; Arachnoidea, such as 4 known spiders (Acarina), such as Argasidae, Ixodidae, and therapeutic worms Sarcopteridae, such as Amblyomma americanum, Amblyomma variegatum, Argas persicus, Boophilus annulatus, Boophilus decoloratus, tiny Boophilus microplus, Dermacentor silvarum, Hyalomma truncatum, Ixodes ricinus, Ixodes rubicundus, Ornithodorus moubata, ear Otobius megnini, Dermanyssus gallinae, Psoroptes ovis, Rhipiceph Alus appendiculatus), Rhipicephalus evertsi, Sarcoptes scabiei, and such as the genus Aculus schlechtendali, Phyllocoptrata oleivora, and Eriophyes sheldoni Eriophyidae spp.; such as the Phytonemus pallidus and the polyphagotarsonemus latus, Tarsonemidae spp.; such as the genus Brevipalus phoenicis Tenuipalidae spp.; such as Tetranychus cinnabarinus, Tetranychus kanzawai, Tetranychus pacificus, Tetranychus telarius, and Tetranychus Urticae), apple red spider 115703.doc -69- 200806642 (Panonychus ulmi), orange genus (Panonychus citri) and grass locust (Oligonychus pratensis) leaf mites (Tetranychidae spp.); 蚤目 (siphonatera ), for example, Xenopsylla cheopis, Ceratophyllus spp. The composition and the compound of formula I are suitable for controlling nematodes, especially plant parasitic nematodes, such as root-knot nematodes, Meloidogyne hapla, Meloidogyne incognita, and Meloidogyne javanica. And other Meloidogyne species; cyst nematodes, Globodera rostochiensis and other Globodera species; Heterodera avenae, Heterodera glycines ), Heterodera schachtii, Heterodera trifolii and other Heterodera species; seed nematodes, Anguina species; stem and leaf nematodes , Aphelenchoides species; chelerythris, Belonolaimus longicaudatus and other Belonolaimus species; pine nematodes, Bursaphelenchus xylophilus and other genus Bursaphelenchus Species; ringworm, Criconema species, ring line (Criconemella) species, Criconemoides species, Mesocriconema species; stem and nematode, Ditylenchus destructor, Ditylenchus dipsaci and other sorghum 115703.doc - 70- 200806642 Ditylenchus species; cone nematodes, Dolichodorus species; spiral nematodes, Helicotylenchus multicinctus and other Helicopterus species; outer sheath nematodes and nematodes Species, Hemicycliophora species and Hemicriconemoides species; Hirschmanniella species; Nematodes, Hoplolaimus species; False root-knot nematodes, Nacobbus species; Nematodes, Longidorus elongatus and other Longidorus species; N. elegans, Paratylenchus species; rot nematodes, Pratylenchus neglectus, northern root rot Nematode (Pratylenchus penetrans), curved root Nematode (Pratylenchus curvitatus), damaged root rot nematode (Pratylenchus goodeyi) and other species of the genus Pratylenchus; locust nematodes, Radopholus similis and other invertebrate species (Radopholus); kidney Nematodes 'Rotylenchus robustus and other Rotylenchus species; Scutellonema species; Residual nematode 'Trichodorus primitivus and other nematodes (Trichodorus) Species, Paratrichodorus species; short nematodes, Tylenchorhynchus claytoni, Tylenchorhynchus dubius and other Dylenchorhynchus species; orange nematodes, nematodes Genus (Tylenchulus) species; sword nematodes, xiphinema species; and other plant-parasitic nematode species. 115703.doc 200806642 In a preferred embodiment of the invention, the compound of formula i is suitable for controlling insects or: known as spiders, especially for lepidoptera, coleopteran and homoptera insects and spiders of the genus . The compounds of the formula I according to the invention are especially suitable for controlling insects of the order Lepidoptera and Homoptera. Formulations therefore, 'the invention further provides an agricultural composition against such animal pests' which comprises the at least one compound of the formula or at least one agriculturally acceptable salt of I and at least one inert liquid having insecticidal action and/or Or a solid agronomically acceptable carrier and, if desired, at least one surfactant. The compositions may contain a single active compound of the formula I or an enantiomer thereof or a mixture of several active compounds I according to the invention. Compositions according to the invention may include individual isomers or mixtures of isomers as well as individual tautomers or mixtures of tautomers. For use in the method according to the invention, the compound I can be converted into conventional formulations such as solutions, emulsions, suspensions, dusts, powders, pastes, granules and solutions which can be directly sprayed. The form of use depends on the specific purpose and application method. The formulations and methods of application are selected to ensure the fine and uniform distribution of the compounds of formula I according to the invention under each condition. Formulations are prepared in a known manner (see, for example, review us 3,060,084, ΕΡ·A 707 445 (for liquid concentrates), Browning, ''Agglomeration'', Chemical Engineering, Dec. 4, 1967 , 147-48, Perry's Chemical Engineer's Handbook, 4th edition, McGraw-Hill, New York, 1963, pp. 8-57 and the following: 115703.doc -72-200806642 WO 91/13546, US 4,172,714, US 4,144,050, US 3,920,442, US 5,180,587, US 5,232,701, US 5,208,030, GB 2,095,558, US 3,299,566, Klingman, Weed Control as a Science, John Wiley and Sons, Inc., New York, 1961, Hance et al. Weed Control Handbook, 8th Edition, Blackwell Scientific Publications, Oxford, 1989 and Mollet, H., Grubemann, A., Formulation technology, Wiley VCH Verlag GmbH, Weinheim (Germany), 2001, 2. DA Knowles, Chemistry and Technology of Agrochemical Formulations, Kluwer Academic Publishers, Dordrecht, 1998 (ISBN 0-7514-0443·8)), for example by injecting active compounds into agriculture Auxiliary agents for chemical formulations, such as solvents and/or carriers, (if required) emulsifiers, surfactants and dispersants, preservatives, defoamers, anti-shock agents, for seed treatment formulations, It is also prepared by incorporating coloring agents and/or binders and/or gelling agents as appropriate. Suitable solvents/carriers are, for example, solvents such as water, aromatic solvents (such as Solvesso products, xylene and the like), paraffins (eg mineral fractions), alcohols (eg sterols, butanol, Pentanol, benzyl alcohol), _ (eg cyclohexyl, decyl-butyrolactone), fluorenone (N-methyl- oxaridone (NMP), N-octylpyrrolidone (NOP)) , acetate (ethylene glycol diacetate), alkyl lactate, lactones such as acena-butyrolactone, ethylene glycol, fatty acid dimethyl decylamine, fatty acids and fatty acid esters, triglycerides, vegetables or Animal source oils and upgraded oils such as alkylated vegetable oils. In principle, a solvent mixture can also be used. 115703.doc •73- 200806642 Carriers, such as ground natural minerals and ground synthetic minerals such as tannins, finely divided tannins, niobates, talc, kaolin, American activated clay, limestone, lime, chalk , red basalt soil, loess, clay, dolomite, diatomaceous earth, calcium sulphate and magnesium sulphate, magnesium oxide, ground synthetic materials such as ammonium sulphate, ammonium sulphate, ammonium sulphate, urea fertilizer and such as mites Powdered meal, bark meal, wood meal and nut shell powder, plant source products of cellulose powder and other solid carriers. Suitable emulsifiers are nonionic and anionic emulsifiers (e.g., polyethylene oxide fatty alcohol ethers, alkyl sulfonates, and aryl sulfonates). Examples of dispersants are lignin sulfite waste liquors and methylcellulose. Suitable surfactants are lignosulfonic acid, naphthalenesulfonic acid, phenolsulfonic acid, alkali metal of dibutylnaphthalenesulfonic acid, alkaline earth metal and ammonium salt, alkyl aryl sulfonate, alkyl sulfate, and burning base. Acid esters, fatty alcohol sulfates, fatty acid and sulfated aliphatic alcohol glycol ethers, in addition to sulfonated naphthalene and naphthalene derivatives and furfural condensate 'naphthalene and hope for formic acid condensate or naphthalene tonic acid Formic acid condensate 'polyethylene oxide octyl phenyl ether, ethoxylated isooctyl phenol, octyl phenol 'nonyl phenol, alkyl phenyl polyglycol ether, tributyl phenyl polyethylene Glycol ether, tristearyl phenyl polyglycol ether, alkyl aryl polyether alcohol, alcohol and fatty alcohol / ethylene oxide condensate, ethoxylated castor oil, polyethylene oxide alkyl ether , ethoxylated polyoxypropylene, lauryl polyethylene glycol ether acetal, sorbitol ester. Further, an anti-agent such as glycerin, ethylene glycol or propylene glycol; an agent such as a bactericide may be added to the formulation. Suitable antifoaming agents are, for example, antifoaming agents based on hydrazine or magnesium stearate. 115703.doc -74- 200806642 Suitable preservatives are, for example, dichlorophenol and benzyl alcohol hemiacetal. Suitable thickeners are compounds which impart a pseudoplastic flow behavior to the formulation, i.e., a viscous viscosity upon standing and a low viscosity during the agitation phase. Mention may be made herein, for example, of commercially available thickeners based on polysaccharides, such as Xanthan

Gum® (來自 Kelco 之 Kelzan®)、Rhodopol® 23(Rhone Poulenc)或 Veegum® (來自 IT· Vanderbilt)，或諸如 Attaclay® (來自Engelhardt)之有機頁矽酸鹽。適用於根據 本發明之分散液之消泡劑為（例如）聚矽氧乳液（諸如來自 Rhodia之 Silikon® SRE、Wacker或 Rhodorsil®)、長鏈醇、 脂肪酸、有機氟化合物及其混合物。可添加殺生物劑以穩 定根據本發明之組合物抵抗微生物之侵襲。適合之殺生物 劑係（例如）基於異噻唑酮，諸如來自Avecia(或Arch)以商 標Proxel®出售或來自Thor Chemie以商標Acticide® RS出 售及來自Rohm &amp; Haas以商標Kathon® MK出售之化合物。 適合之防東劑為有機多元醇，例如乙二醇、丙二醇或甘 油。以活性化合物組合物之總重量計，該等者係通常以不 大於10重量％之量來使用。若適當，則根據本發明之活性 化合物組合物可包括以所製備之調配物之總量計1至5重量 %之緩衝液以調節pH值，所使用緩衝液之量及類型視活性 化合物之化學性質而定。緩衝液之實例為諸如磷酸、g朋 酸、乙酸、丙酸、檸檬酸、反丁烯二酸、酒石酸、草酸及 丁二酸之弱無機酸或弱有機酸之驗金屬鹽。 適合於製備可直接喷霧之溶液、乳液、糊狀物或油分散 液之物質為諸如煤油或柴油之中至高沸點之礦物油餾份、 115703.doc -75- 200806642 此外煤焦油及植物或動物源油，例如曱苯、二甲笨、石 蠟、四氳萘、烷基化萘或其衍生物之脂族烴、環烴及芳族 烴’甲醇、乙醇、丙醇、丁醇、環己醇、環己_、異佛爾 酮，例如二甲亞砜、N_甲基吡咯啶酮及水之強極性溶劑。 粉末、用於撒布之材料及微塵可藉由將活性物質與固體 載劑混合或同時研磨來製備。 例如包衣顆粒、浸潰顆粒及均質顆粒之顆粒可藉由將活 性成份與固體載劑結合來製備。固體載劑之實例為諸如矽 膠、矽酸鹽、滑石粉、高嶺土、美國活性白土、石灰石、 石灰、白堊、紅玄武土、黃土、黏土、白雲石、矽藻土' 硫酸鈣、硫酸鎂、氧化鎂、經研磨之合成物質之礦物土， 諸如硫酸銨、磷酸銨、硝酸銨、尿素之肥料，及諸如穀類 粕粉、樹皮粕粉、木材粕粉及堅果殼粕粉、纖維素粉末之 植物源產品及其他固體載劑。 一般而言，調配物包括0_01至95重量％，較佳〇1至9〇重 量％之活性成份。該等活性成份係以9〇%至1〇〇%之純度， 較佳95%至1〇〇%之純度（根據NMR譜）來使用。 對種子處理目的而言，各別調配物可稀釋2_1〇倍並在即 用製劑中產生以活性化合物重量計0.01至6〇重量％，較佳 0.1至40重量。/〇之濃度。 式I化合物可藉助於喷霧、霧化、撒粉、撒布或洗注而 如此以其調配物形式或以自其製備之使用形式來使用，例 如以可直接喷霧之溶液、粉末、懸浮液或分散液、乳液、 油分散液、糊狀物、可撒粉之產品、用於撒布之材料或顆 115703.doc • 76- 200806642 粒形式來使用。該等使用形式完全視所欲之目的而定；希 望其在各狀況下確保根據本發明之活性化合物之最精細可 能分佈。 水性使用形式可藉由添加水而自乳液濃縮物、糊狀物或 可濕性粉末（可噴霧粉末、油分散液）來製備。為製備乳 液、糊狀物或油分散液，該等或溶於油或溶劑中之物質， 可藉助於濕潤劑、增黏劑、分散劑或乳化劑而在水中均質 化。或者，可能製備包括活性物質、濕潤劑、增黏劑、分 政州或乳化鈉及（若適當）溶劑或油之濃縮物，且該等濃縮 物適於以水稀釋。 即用產品中之活性成份濃度可在相對廣之範圍内變化。 一般而言，其為〇.〇〇〇1至1〇重量％，較佳為〇〇1至1重量 %。 活性成份亦可成功地用於超低容量方法（ULV)中，可能 應用包括超過95重量％之活性成份之調配物，或甚至可能 應用無添加劑之活性成份。 以下為調配物之實例： L用於以水稀釋之產品。對種子處理目的而言，該等產 品可施用於經稀釋或未經稀釋之種子。 A)水溶性濃縮物（SL、ls) 將10重量份之活性化合物溶於9〇重量份之水或水溶性溶 d中作為替代方法，添加濕潤劑或其他助劑。在用水稀 釋後，活性化合物溶解，藉以獲得具有1〇% (w/w)之活性 化合物之調配物。 115703.doc -77- 200806642 B) 可分散性濃縮物（DC) 將20重量份之活性化合物溶於70重量份之環己酮中，同 時添加1G重量份之例如聚乙烯t各相之分散劑。用水稀 釋付到为散液’藉以獲付具有20% (w/w)之活性化合物之 調配物。 C) 可乳化濃縮物（EC) 將15重量份之活性化合物溶於7重量份之二甲苯中，同 時添加十二烷基苯磺酸鈣及蓖麻油乙氧基化物（每種為5重 量份）。用水稀釋得到乳液，藉以獲得具有15% (w/w)之活 性化合物之調配物。 D) 乳液（EW、EO、ES) 將25重量份之活性化合物溶於35重量份之二甲苯中，同 時添加十二烷基苯磺酸鈣及蓖麻油乙氧基化物（每種為5重 量份）。藉助於乳化機（例如Ultraturax)將該混合物引入至 30重量份之水中且製成均質乳液。用水稀釋得到乳液，藉 以獲得具有25% (w/w)之活性化合物之調配物。 E) 懸浮液（SC、〇D、FS) 在攪動式球磨機中，將20重量份之活性化合物粉碎，同 時添加10重量份之分散劑、濕潤劑及70重量份之水或有機 溶劑以得到精細活性化合物懸浮液。用水稀釋得到活性化 合物之穩定懸浮液，藉以獲得具有20% (w/w)之活性化合 物之調配物。 F) 水可分散性顆粒及水溶性顆粒（WG、SG) 將5 0重量份之活性化合物精細研磨，同時添加5 〇重量份 115703.doc -78- 200806642 之分散劑及濕潤劑且藉助於工業設備（例如擠壓機、喷霧 土合、流體化床）製成水可分散性或水溶性顆粒。用水稀釋 付到活性化合物之穩定分散液或溶液，藉以獲得具有50〇/〇 (W/W)之活性化合物之調配物。 G) 水可分散性粉末及水溶性粉末（Wp ' sp、ss、ws) 在轉子-定子型研磨機中研磨75重量份之活性化合物， 同時添加25重量份之分散劑、濕潤劑及矽膠。用水稀釋得 到活性化合物之穩定分散液或溶液，藉以獲得具有75% (w/w)之活性化合物之調配物。 H) 凝膠調配物（GF) 在攪動式球磨機中，將20重量份之活性化合物粉碎，同 時添加10重量份之分散劑、丨重量份之膠凝劑濕潤劑及7〇 重里份之水或有機溶劑以得到精細活性化合物懸浮液。用 水稀釋得到活性化合物之穩定懸浮液，藉以獲得具有 (w/w)之活性化合物之調配物。 2·欲不稀釋而應用於葉應用之產品。對種子處理目的而 s，该等產品可施用於經稀釋或未經稀釋之種子。 I) 可撒粉之粉末（DP、DS) 將5重i份之活性化合物精細研磨且與9 5重量份之細粉 狀高嶺土密切混合。此得到具有5% (w/w)之活性化合物之 可撒粉產品。 J) 顆粒（GR、FG、GG、MG) 將0 · 5重里伤之活性化合物精細研磨且與&amp; $ · $重量份之載 劑結合，藉以獲得具有0.5。/。（w/w)之活性化合物之調配 115703.doc -79- 200806642 此得到欲不 物。當前方法為擠壓、喷霧乾燥或流體化床 稀釋而應用於葉用途之顆粒。 K)ULV溶液（UL) 重量份之例如二甲苯之 用於葉用途之具有10〇/〇 將10重量份之活性化合物溶於9〇 有機溶劑中。此得到不經稀釋而應 (W/W)之活性化合物的產品。 各種類型之油、濕潤劑、佐劑、除草劑、殺直立 他殺蟲劑或殺_可添加至活性成份中，:a二使 用前f接添加(槽式混合)。該等藥劑通常係以:二 之重里比與根據本發明之藥劑混合。 本發明化合物！之化合物及組合物可與其他活性成份一 :應用，例如與其他殺蟲劑，殺昆蟲劑，除草劑，諸如石肖 尿素、鉀鹼及過磷酸鹽之肥料，植物毒素及植物生 長调即^ *全劑及殺線蟲劑—起應用。該等額外成份可 依序使用或與上文所描述之組合物組合使用，若適當，亦 僅在使用則直接添加（槽式混合）。舉例而言，可在用其他 活性成份處理前或處理後，用本發明之組合物喷灑植物。 該等額外活性藥劑可以1:1〇至1〇:1之重量比與根據本發 明所使用之藥劑混合。將呈使用形式之化合物！或包括其 之組口物作為殺蟲劑頻t地與其他殺蟲劑混纟而產生更廣 泛的殺蟲作用範圍。 一心欲以下列可與根據本發明化合物連用及可產生潛在協 同效應之殺蟲劑清單Μ，說明可能之組合，但不強加任何 限制： 115703.doc 200806642 Μ· 1 ·有機（硫代）麟酸g旨：歐殺松（acephate)、亞滅松 (azamethiphos)、榖硫磷（azinphos-methyl)、陶斯松 (chlorpyrifos)、曱基陶斯松（chlorpyrifos-methyl)、毒蟲畏 (chlorfenvinphos)、大利松（diazinon)、敵敵畏 (dichlorvos)、雙特松（dicrotophos)、大滅松（dimethoate)、 二硫松（disulfoton)、 愛殺松（ethion)、撲滅松 (fenitrothion)、芬殺松（fenthi〇n)、異号殺松（isoxathion)、 馬拉松（malathion)、曱胺石粦（methamidophos)、滅大松 (methidathion)、曱基對硫磷（methyl-parathion)、美文松 (mevinphos)、亞素靈（monocrotophos)、滅多松 (oxydemeton-methyl)、雙氧填（paraoxon)、對硫填 (parathion)、賽達松（phenthoate)、裕必松（phosalone)、益 滅松（phosmet)、福賜米松（phosphamidon)、福瑞松 (phorate)、巴賽松（phoxim)、亞特松（pirimiphos-methyl)、 布飛松（profenofos)、普硫松（prothiofos)、殺普松 (sulprophos)、殺蟲畏（tetrachlorvinphos)、託福松 (terbufos)、三嗤構（triazophos)、三氣松（trichlorfon); Μ·2.胺基甲酸酯：阿蘭克（alanycarb)、得滅克 (aldicarb)、免敵克（bendiocarb)、本夫克（benfuracarb)、加 保利（carbaryl)、加保扶（carbofuran)、丁基加保扶 (carbosulfan)、芬氧克（fenoxycarb)、夫硫克 (furathiocarb)、滅賜克（methiocarb)、滅多蟲（methomyl)、 歐殺滅（oxamyl)、抗财威（pirimicarb)、殘殺威（propoxur)、 硫地克（thiodicarb)、嗤坊威（triazamate); 115703.doc -81- 200806642 M.3.擬除蟲菊酯：丙稀除蟲菊（allethrin)、畢芬寧 (bifenthrin)、賽扶寧（cyfluthrin)、赛洛寧（cyhalothrin)、賽 紛寧（cyphenothrin)、賽滅寧（cypermethrin)、亞滅寧 (alpha-cypermethrin)、高效氣氰菊醋（beta_cypermethrin)、 ζ-氣氰菊酯（zeta-cypermethrin)、第滅寧（deltamethrin)、益 避寧（empenthrin)、益化利（esfenvalerate)、依芬寧 (etofenprox)、芬普寧（fenpropathrin)、芬化利 (fenvalerate)、依普寧（imiprothrin)、λ-賽洛寧（lambda-cyhalothrin)、百滅寧（permethrin)、普亞列寧 (prallethrin)、除蟲菊精 I及 II(pyrethrin I and II)、異列滅寧 (resmethrin)、氟石夕菊酯（silafluofen)、氟胺氰菊酯（tau-fluvalinate)、七氟菊 δ旨(tefluthrin)、治滅寧 (tetramethrin)、四漠菊酉旨(tralomethrin)、拜富寧 (transfluthrin)、丙氟菊醒（profluthrin)、四氟甲鱗菊酉旨 (dimefluthrin)； Μ.4.生長調節劑：a)甲殼素合成抑制劑：苯曱醯基脲： 克福隆（chlorfluazuron)、二福隆（diflubenzuron)、氟環脲 (flucycloxuron)、氟芬隆（flufenoxuron)、六伏隆 (hexaflumilron)、祿芬隆（lufenuron)、諾華隆（novaluron)、 得福隆（teflubenzuron)、殺蟲隆（triflumuron);布芬淨 (buprofezin)、戴芬蘭（diofenolan)、合賽多（hexythiazox)、 乙虫茜°坐（etoxazole)、克芬蜗（clofentazine) ; b)蜆皮激素拮 抗劑：氣蟲醢肼（halofenozide)、 甲氧蟲醯肼 (methoxyfenozide)、蟲醯肼（tebufenozide)、印楝素 115703.doc -82 - 200806642 (azadirachtin) ; c)類幼年素：比普西芬（pyriproxyfen)、美 賜年（methoprene)、芬氧克（fenoxycarb) ; d)脂質生物合成 抑制劑：螺二克芬（spirodiclofen)、斯必麥芬（spiromesifen)、 斯必馬特（spirotetramat); M.5.菸鹼受體促效劑/拮抗劑化合物：可尼丁 (clothianidin)、達特南（dinotefuran)、益達胺 (imidacloprid)、嗟蟲嗓（thiamethoxam)、尼藤 σ比藍 (nitenpyram)、亞滅培（acetamiprid)、σ塞蟲琳（thiacloprid) 及 AKD-1022 ; M.6.GABA拮抗劑化合物：乙醯普羅（acetoprole)、硫丹 (endosulfan)、乙蟲清（ethiprole)、氟蟲腈（fipronil)、凡尼 普羅（vaniliprole)、11比氟普羅（pyrafluprole)、°比普羅 (pyriprole)、式Γ2之苯基σ比嗤化合物Gum® (Kelzan® from Kelco), Rhodopol® 23 (Rhone Poulenc) or Veegum® (from IT Vanderbilt), or organic phthalate such as Attaclay® (from Engelhardt). Antifoaming agents suitable for use in the dispersions according to the invention are, for example, polyoxyxides (such as Silikon® SRE, Wacker or Rhodorsil® from Rhodia), long chain alcohols, fatty acids, organofluorine compounds and mixtures thereof. A biocide can be added to stabilize the composition according to the invention against microbial attack. Suitable biocides are, for example, based on isothiazolone, such as those sold under the trademark Proxel® from Avecia (or Arch) or sold under the trademark Acticide® RS from Thor Chemie and sold under the trademark Kathon® MK by Rohm &amp; Haas. . Suitable anti-agents are organic polyols such as ethylene glycol, propylene glycol or glycerin. These are usually used in an amount of not more than 10% by weight based on the total weight of the active compound composition. If appropriate, the active compound composition according to the invention may comprise from 1 to 5% by weight, based on the total amount of the formulation prepared, to adjust the pH, the amount of buffer used and the type of chemistry of the active compound. Nature depends. Examples of the buffer are metal salts of weak inorganic acids or weak organic acids such as phosphoric acid, g-p-acid, acetic acid, propionic acid, citric acid, fumaric acid, tartaric acid, oxalic acid and succinic acid. A substance suitable for the preparation of a solution, emulsion, paste or oil dispersion which can be directly sprayed is a mineral oil fraction such as kerosene or diesel which is at a high boiling point, 115703.doc -75-200806642 Further coal tar and plants or animals Source oils, such as terpene, dimethyl, paraffin, tetraterpene, alkylated naphthalene or derivatives thereof, aliphatic hydrocarbons, cyclic hydrocarbons and aromatic hydrocarbons 'methanol, ethanol, propanol, butanol, cyclohexanol , cyclohexanyl, isophorone, such as dimethyl sulfoxide, N-methylpyrrolidone and a strong polar solvent of water. Powders, materials for spreading and fine dust can be prepared by mixing or simultaneously grinding the active material with a solid carrier. For example, coated granules, impregnated granules, and granules of homogeneous granules can be prepared by combining the active ingredient with a solid carrier. Examples of solid carriers are, for example, tannin, citrate, talc, kaolin, American activated clay, limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth 'calcium sulfate, magnesium sulfate, oxidation Magnesium, mineralized soil of ground synthetic materials, fertilizers such as ammonium sulfate, ammonium phosphate, ammonium nitrate, urea, and plant sources such as cereal meal, bark meal, wood meal and nut meal, cellulose powder Products and other solid carriers. In general, the formulation comprises from 0 to 01% by weight, preferably from 1 to 9% by weight of active ingredient. The active ingredients are used in a purity of from 9 to 1% by weight, preferably from 95% to 1% by weight (according to NMR spectrum). For seed treatment purposes, the individual formulations may be diluted 2 to 1 fold and produce from 0.01 to 6 weight percent, preferably from 0.1 to 40 weight percent, by weight of the active compound in the ready-to-use formulation. / concentration of 〇. The compounds of the formula I can be used in the form of their formulations or in the form in which they are prepared by spraying, atomizing, dusting, spreading or washing, for example in the form of directly sprayable solutions, powders, suspensions Or dispersions, emulsions, oil dispersions, pastes, dusting products, materials for spreading or pellets of 115703.doc • 76-200806642. These forms of use depend entirely on the intended purpose; it is intended to ensure the finest possible distribution of the active compounds according to the invention in each case. The aqueous use form can be prepared from an emulsion concentrate, a paste or a wettable powder (sprayable powder, oil dispersion) by adding water. For the preparation of emulsions, pastes or oil dispersions, such materials which are soluble in oils or solvents can be homogenized in water by means of wetting agents, tackifiers, dispersants or emulsifiers. Alternatively, it is possible to prepare a concentrate comprising an active substance, a wetting agent, a tackifier, a sub-state or an emulsified sodium and, if appropriate, a solvent or oil, and such concentrates are suitable for dilution with water. The concentration of the active ingredient in the ready-to-use product can vary over a relatively wide range. In general, it is from 1 to 1% by weight, preferably from 1 to 1% by weight. The active ingredient can also be used successfully in ultra low volume methods (ULV), possibly with formulations comprising more than 95% by weight of the active ingredient, or even the use of active ingredients without additives. The following are examples of formulations: L is for products diluted with water. For seed treatment purposes, such products can be applied to diluted or undiluted seeds. A) Water-soluble concentrate (SL, ls) 10 parts by weight of the active compound is dissolved in 9 parts by weight of water or water-soluble solution d as an alternative method, and a wetting agent or other auxiliary agent is added. After dilution with water, the active compound is dissolved to obtain a formulation having 1% (w/w) of active compound. 115703.doc -77- 200806642 B) Dispersible Concentrate (DC) 20 parts by weight of the active compound are dissolved in 70 parts by weight of cyclohexanone while adding 1 G by weight of a dispersing agent such as polyethylene t phase . Formulation of a 20% (w/w) active compound is obtained by diluting with water to a dispersion. C) Emulsifying concentrate (EC) 15 parts by weight of the active compound are dissolved in 7 parts by weight of xylene with addition of calcium dodecylbenzenesulfonate and castor oil ethoxylate (5 parts each) ). The emulsion was diluted with water to obtain a formulation having 15% (w/w) of the active compound. D) Emulsion (EW, EO, ES) 25 parts by weight of active compound is dissolved in 35 parts by weight of xylene with addition of calcium dodecylbenzenesulfonate and castor oil ethoxylate (5 weight each) Share). The mixture was introduced into 30 parts by weight of water by means of an emulsifier (e.g., Ultraturax) and a homogeneous emulsion was prepared. The emulsion is diluted with water to obtain a formulation having 25% (w/w) of the active compound. E) Suspension (SC, 〇D, FS) In an agitated ball mill, 20 parts by weight of the active compound is pulverized while adding 10 parts by weight of a dispersant, a wetting agent and 70 parts by weight of water or an organic solvent to obtain a fine Active compound suspension. Dilution with water gives a stable suspension of the active compound to obtain a formulation having 20% (w/w) of active compound. F) Water-dispersible granules and water-soluble granules (WG, SG) 50 parts by weight of the active compound are finely ground while adding 5 parts by weight of the dispersant and humectant of 115703.doc-78-200806642 and by means of industry Equipment such as extruders, spray soils, fluidized beds are made of water-dispersible or water-soluble particles. Dilution with water is carried out to obtain a stable dispersion or solution of the active compound to obtain a formulation having an active compound of 50 Å/W (W/W). G) Water-dispersible powder and water-soluble powder (Wp 'sp, ss, ws) 75 parts by weight of the active compound are ground in a rotor-stator type grinder while adding 25 parts by weight of a dispersing agent, a wetting agent and a silicone rubber. Dilution with water gives a stable dispersion or solution of the active compound to obtain a formulation having 75% (w/w) of active compound. H) Gel Formulation (GF) In an agitated ball mill, 20 parts by weight of the active compound is pulverized while adding 10 parts by weight of a dispersing agent, a by weight of a gelling agent wetting agent and 7 parts by weight of water or The organic solvent is used to obtain a suspension of the fine active compound. Dilution with water gives a stable suspension of the active compound in order to obtain a formulation of the active compound (w/w). 2. Products intended for leaf application without dilution. For seed treatment purposes, these products can be applied to diluted or undiluted seeds. I) Powder which can be dusted (DP, DS) Five parts by weight of the active compound are finely ground and intimately mixed with 95 parts by weight of fine powdery kaolin. This gave a dustable product having 5% (w/w) of active compound. J) Granules (GR, FG, GG, MG) The 0.5 kg of the active compound is finely ground and combined with &amp; $· parts by weight of the carrier to obtain 0.5. /. (w/w) compounding of active compounds 115703.doc -79- 200806642 This is not desired. Current methods are granules for leaf applications that are extruded, spray dried or fluidized bed dilution. K) ULV solution (UL) parts by weight of, for example, xylene having 10 Å/〇 for leaf use 10 parts by weight of the active compound are dissolved in 9 〇 organic solvent. This gives the product of the active compound (W/W) which is not diluted. Various types of oils, humectants, adjuvants, herbicides, erectile insecticides or sputum can be added to the active ingredient, a: two before use f addition (tank mixing). Such agents are typically mixed with a medicament according to the invention at a weight ratio of two. The compound of the invention! The compounds and compositions can be used in combination with other active ingredients: for example, with other insecticides, insecticides, herbicides, fertilizers such as scutellaria urea, potash and perphosphate, plant toxins and plant growth regulators ^ * Full dose and nematicide - for applications. These additional ingredients may be used sequentially or in combination with the compositions described above, and if appropriate, added directly (tank mix). For example, the plants can be sprayed with the compositions of the present invention before or after treatment with other active ingredients. The additional active agents may be mixed with the agent used in accordance with the present invention in a weight ratio of from 1:1 Torr to 1 Torr:1. Will be in the form of a compound! Or a group of mouthpieces thereof, as insecticides, are mixed with other insecticides to produce a broader range of insecticidal action. It is intended to illustrate the possible combinations with the following list of pesticides which can be used in combination with the compounds according to the invention and which can produce a potential synergistic effect, without imposing any restrictions: 115703.doc 200806642 Μ· 1 ·Organic (thio) linonic acid g Purpose: acephate, azamethiphos, azinphos-methyl, chlorpyrifos, chlorpyrifos-methyl, chlorfenvinphos, dansson ( Diazinon), dichlorvos, dicrotophos, dimethoate, disulfoton, ethion, fenitrothion, fenthi〇n , isoxathion, malathion, methamidophos, methidathion, methyl-parathion, mevinphos, monocrotophos ), oxydemeton-methyl, paraoxon, parathion, phenthoate, phosalone, phosmet, phosphamidon ), Phosphon, phoxim, pirimiphos-methyl, profenofos, prothiofos, sulprophos, tetrachlorvinphos, tofusone (terbufos), triazophos, trichlorfon; Μ·2. urethane: alanycarb, aldicarb, bendiocarb, Benf Benfuracarb, carbaryl, carbofuran, carbosulfan, fenoxycarb, furathiocarb, metiocarb, worms (methomyl), oxamyl, pirimicarb, propoxur, thiodicarb, triazamate; 115703.doc -81- 200806642 M.3. Pyrethrins: allethrin, bifenthrin, cyfluthrin, cyhalothrin, cyphenothrin, cypermethrin, arsenin (alpha-cypermethrin), high-efficiency beta-cypermethrin, ζ-cymidine (zeta-cypermethrin), deltamethrin, empenthrin, esfenvalerate, etofenprox, fenpropathrin, fenvalerate, epretin ( Imiprothrin), lambda-cyhalothrin, permethrin, prallethrin, pyrethrin I and II, resmethrin, Silafluofen, tau-fluvalinate, tefluthrin, tetramethrin, trolomethrin, transfluthrin ), profluthrin, dimefluthrin; Μ.4. growth regulator: a) chitin synthesis inhibitor: phenylhydrazine urea: chlorfluazuron, Diflubenzuron, flucycloxuron, flufenoxuron, hexaflumilron, lufenuron, novaluron, teflubenzuron, insecticide Triflumuron; buprofezin, dafino Lan), hexythiazox, etoxazole, clofentazine; b) ecdysone antagonist: halofenozide, methoxyfenozide , insect (tebufenozide), azadirachtin 115703.doc -82 - 200806642 (azadirachtin); c) juveniles: pyriproxyfen (methoprene), fenoxycarb (fenoxycarb); d) Lipid biosynthesis inhibitors: spirodiclofen, spiromesifen, spirotetramat; M.5. nicotinic receptor agonist/antagonist compound: coney Ding (clothianidin), dinotefuran, imidacloprid, thiamethoxam, nitenpyram, acetamiprid, thiacloprid and AKD-1022; M.6. GABA antagonist compounds: acetoprole, endosulfan, ethiprole, fipronil, vaniliprole, 11 specific fluoride Pyrofluprole, pyriprole, phenyl σ 嗤Compound

〇 S〇 S

Μ.7.巨環内酯殺昆蟲劑：阿巴汀（abamectin)、因滅汀 (emamectin)、密滅汀（milbemectin)、來匹美 丁 (lepimectin)、賜諾殺（spinosad); M.8. METI I化合物：芬那劄奎（fenazaquin)、比達本 (pyridaben)、得布芬比（tebufenpyrad)、嗤蟲酸胺 (tolfenpyrad)、I 芬林（flufenerim); 115703.doc -83- 200806642 Μ·9· ΜΕΤΙ II及 III化合物：阿色奎西（acequinocyl)、氟 西比林（fluacyprim)、伏蟻脎（hydramethylnon); Μ· 10·非偶聯劑化合物：克芬那比（chlorfenapyr); Μ·11·氧化構酸化抑制劑化合物：環己錫（cyhexatin)、汰 芬隆（diafenthiuron)、芬布賜（fenbutatin oxide)、歐虫高多 (propargite)； Μ· 12.蜆皮中斷劑化合物：賽滅淨（cyromazine); M.13.混合作用氧化酶抑制劑化合物：協力精（piperonyl butoxide)； ]\4.14.鈉通道阻斷劑化合物：因得克（丨11〇1〇乂&amp;031：13)、美氟 月宗（metaflumizone); Μ. 15.以下各種：三亞蜗（amitraz)、 苯氣嗟 (benclothiaz)、畢芬載（bifenazate)、培丹（cartap)、氟尼胺 (flonicamid)、咬蟲丙醚（pyridalyl)、比美卓秦 (pymetrozine)、硫、殺蟲環（thiocyclam)、氟苯二醢胺 (flubendiamide)、σ塞嗜口辰芬（cyenopyrafen)、氟 °比 σ坐福斯 (flupyrazofos)、嗟氟美芬（cyflumetofen)、胺氣美 (amidoflumet)、比氣喧吐（pyrifluquinazon)、式 Γ4之胺基口轰 唆琳酮化合物Μ.7. Macrolide insecticide: abamectin, emamectin, milbemectin, lepimectin, spinosad; M. 8. METI I compounds: fenazaquin, pyridaben, tebufenpyrad, tolfenpyrad, flufenerim; 115703.doc -83- 200806642 Μ·9· ΜΕΤΙ Compounds II and III: acequinocyl, fluacyprim, hydramethylnon; Μ·10·non-coupling compound: chlorfenapyr ;·11·Oxidation acidification inhibitor compounds: cyhexatin, diafenthiuron, fenbutatin oxide, propargite; Μ·12. Compound: cyromazine; M.13. Mixed action oxidase inhibitor compound: piperonyl butoxide; ]\4.14. Sodium channel blocker compound: Indek (丨11〇1〇乂&amp;031:13), metaflumizone; Μ. 15. The following various types: amitraz, benzene Benbenziaz, bifenazate, cartap, flonicamid, pyridalyl, pymetrozine, sulfur, thiocyclam, Flubendiamide, cyenopyrafen, flupyrazofos, cyflumetofen, amidoflumet, specific gas vomiting Pyrifluquinazon), an amine-based ketone compound of formula Γ4

(Γ4)， N-R’-2,2-二鹵基-1-11&quot;環-丙烷羧醯胺-2-(2,6-二氯-α，α，α- 115703.doc -84- 200806642 三-氟-對甲苯基）腙或N-R’-2,2-二（Rm)丙醯胺-2-(2,6-二氣-α，α，α-三氟-對甲苯基）-腙，其中R’為甲基或乙基，鹵基為 氣基或溴基，RM為氫或曱基且R…為曱基或乙基，如 chlorantraniliprole或式Γ5化合物之鄰胺基苯曱酸醯胺化 合物(Γ4), N-R'-2,2-dihalo-1-11&quot;cyclopropanecarboxamide-2-(2,6-dichloro-α,α,α- 115703.doc -84- 200806642 Tri-fluoro-p-tolyl) oxime or N-R'-2,2-di(Rm)propanamide-2-(2,6-di-gas-α,α,α-trifluoro-p-tolyl -腙, wherein R' is methyl or ethyl, halo is a gas or bromo group, RM is hydrogen or fluorenyl and R is a fluorenyl or ethyl group, such as chlorantraniliprole or anthranilic benzene of a compound of formula Γ5 Indole amide compound

CH 厂 fj 及如描述於 JP 2002 284608、WO 02/89579、WO 02/ 90320 &gt; WO 02/90321、WO 04/06677、WO 04/20399、JP 2004 99597、WO 05/68423、WO 05/68432或 WO 05/63694 中之丙二腈化合物，尤其為丙二腈化合物 CF3(CH2)2C(CN)2CH2(CF2)3CF2H、CF3(CH2)2C(CN)2CH2 (cf2)5cf2h、cf3(ch2)2c(cn)2(ch2)2c(cf3)2f、cf3(ch2)2 c(cn)2(ch2)2(cf2)3cf3、cf2h(cf2)3ch2c(cn)2ch2(cf2)3 cf2h、cf3(ch2)2c(cn)2ch2(cf2)3cf3、cf3(cf2)2ch2c (cn)2ch2(cf2)3cf2h及 cf3cf2ch2c(cn)2ch2(cf2)3cf2h。CH plant fj and as described in JP 2002 284608, WO 02/89579, WO 02/90320 &gt; WO 02/90321, WO 04/06677, WO 04/20399, JP 2004 99597, WO 05/68423, WO 05/68432 Or the malononitrile compound in WO 05/63694, especially the malononitrile compound CF3(CH2)2C(CN)2CH2(CF2)3CF2H, CF3(CH2)2C(CN)2CH2 (cf2)5cf2h, cf3(ch2) 2c(cn)2(ch2)2c(cf3)2f, cf3(ch2)2 c(cn)2(ch2)2(cf2)3cf3, cf2h(cf2)3ch2c(cn)2ch2(cf2)3 cf2h, cf3( Ch2) 2c (cn) 2ch2 (cf2) 3cf3, cf3 (cf2) 2ch2c (cn) 2ch2 (cf2) 3cf2h and cf3cf2ch2c (cn) 2ch2 (cf2) 3cf2h.

市售之群M化合物可見於The Pesticide Manual，第13 版，British Crop Protection Council (2003)連同其他公開 案中。式Γ2之硫代醯胺及其製備已描述於wo 98/28279 中。來匹美汀自 Agro Project，PJB Publications Ltd， November 2004已知。苯氣噻及其製備已描述於eP-AI 115703.doc -85 - 200806642 454621中。滅大松及雙氧磷及其製備已描述於Farm Chemicals Handbook, Volume 88, Meister Publishing Company，2001中。乙醯普羅及其製備已描述於WO 98/ 28277中。美氟腙及其製備已描述於EP-A1 462 456中。氟 吡唑福斯已描述於 Pesticide Science 54，1988，第 237-243 頁中及US 4822779中。吡氟普羅及其製備已描述於JP 2002193709中及WO 01/00614中。吡普羅及其製備已描述 於WO 98/45274中及US 6335357中。胺氟美及其製備已描 述於US 6221890中及JP 21010907中。氟芬林及其製備已描 述於WO 03/007717中及WO 03/007718中。噻氟美芬及其 製備已描述於WO 04/080180中。式Γ4之胺基喹唑啉酮化合 物已描述於EPA 109 7932中。Commercially available Group M compounds can be found in The Pesticide Manual, 13th Edition, British Crop Protection Council (2003), among other publications. The thioguanamine of the formula 及其2 and its preparation have been described in WO 98/28279. Leipin is known from Agro Project, PJB Publications Ltd, November 2004. Benzophenone and its preparation have been described in eP-AI 115703.doc-85 - 200806642 454621. Damascus and bisphosphonate and their preparation have been described in Farm Chemicals Handbook, Volume 88, Meister Publishing Company, 2001. Ethidium and its preparation have been described in WO 98/28277. Methotrexate and its preparation have been described in EP-A1 462 456. Fluoropyrazols has been described in Pesticide Science 54, 1988, pages 237-243 and US 4822779. Pyriprazine and its preparation have been described in JP 2002193709 and in WO 01/00614. Pyrprom and its preparation are described in WO 98/45274 and in US Pat. No. 6,335,357. Amine fluoroamine and its preparation are described in US 6221890 and JP 21010907. Flufenillin and its preparation are described in WO 03/007717 and in WO 03/007718. Tetfluramine and its preparation have been described in WO 04/080180. The amine quinazolinone compounds of formula 已4 have been described in EPA 109 7932.

式Γ5之鄰胺基苯甲酸醯胺及其製備已描述於WO 01/70671 ； WO 02/48137 ； WO 03/24222 &gt; WO 03/15518、 WO 04/67528 ; WO 04/33468 ;及 WO 05/118552 中。丙二 腈化合物 CF3(CH2)2C(CN)2CH2(CF2)3CF2H、CF3(CH2)2C (cn)2ch2(cf2)5cf2h、cf3(ch2)2c(cn)2(ch2)2c(cf3)2f、 cf3(ch2)2c(cn)2(ch2)2(cf2)3cf3、cf2h(cf2)3ch2c(cn)2 ch2(cf2)3cf2h、cf3(ch2)2c(cn)2ch2(cf2)3cf3、cf3(cf2)2 ch2c(cn)2ch2(cf2)3cf2h 及 cf3cf2ch2c(cn)2ch2(cf2)3 CF2H已描述於WO 05/63694中。 殺真菌混合搭配物為選自由以下物質組成之群F之彼等 者： F.1醯基丙胺酸類，諸如苯霜靈（benalaxyl)、滅達樂 115703.doc -86 - 200806642 (metalaxyl)、吱醯胺（ofurace)、歐殺斯（oxadixyl); F.2胺衍生物，諸如阿迪嗎琳（aldimorph)、多寧 (dodine)、嗎菌靈（dodemorph)、粉鏽琳（fenpropimorph)、 苯鐵°定（fenpropidin)、雙胍鹽（guazatine)、雙脈辛胺 (iminoctadine)、螺惡胺（spiroxamine)、三得芬 (tridemorph)； F.3苯胺基嘴咬類，諸如比利美沙尼（pyrimethanil)、米 潘尼比林（mepanipyrim)或賽普洛（cyprodinyl); F.4抗生素，諸如環己醯亞胺、灰黃黴素（griseofulvin)、 春曰黴素（kasugamycin)、遊黴素（natamycin)、多氧菌素 (polyoxin)或鏈黴素（streptomycin); F.5。坐類，諸如比多農（bitertanol)、 溴克座 (bromoconazole)、環克座（cyproconazole)、苯醚甲環唾 (difenoconazole)、二硝基克嗤（dinitroconazole)、氟環嗤 (epoxiconazole)、芬克座(fenbuconazole) 、 I 啥 σ坐 (fluquinconazole)、護石夕得（flusilazole)、己嗤醇 (hexaconazole)、依滅歹，J (imazalil)、葉菌口坐（metconazole)、 邁克尼（myclobutanil)、平克座（penconazole)、普克利 (propiconazole)、撲克拉（prochloraz)、丙硫醇克嗤 (prothioconazole)、得克利（tebuconazole)、三泰芬 (triadimefon)、三泰隆（triadimenol)、賽福座 (triflumizole)、環菌 11 坐(triticonazole)、護汰芬 (flutriafol); F.6二羧甲醯亞胺類，諸如依普同（iprodion)、米克啉 115703.doc -87- 200806642 (myclozolin)、撲滅寧（procymidon)、免克寧（vinclozolin); F.7二硫代胺基甲酸i旨類，諸如福美鐵（ferbam)、代森鈉 (nabam)、猛乃浦（maneb)、锰粉克（mancozeb)、威百故 (metam)、免得爛（metiram)、甲基辞乃浦（propineb)、聚胺 基甲酸醋（polycarbamate)、得恩地（thiram)、益穗（ziram)、 鋅乃浦（zineb); F.8雜環化合物，諸如敵菌靈（anilazine)、免賴得 (benomyl)、博克利（boscalid)、貝芬替（carbendazim)、萎 鏽靈（carboxin)、氧化萎鏽靈（oxycarboxin)、賽座滅 (cyazofamid)、邁隆（dazomet)、二硫二氰蒽 g昆（dithianon)、 口惡σ坐菌顚I (famoxadone)、口米σ坐菌酮（fenamidone)、芬瑞莫 (fenarimol)、麥穗靈（fuberidazole)、說多寧（flutolanil)、 福拉比（furametpyr)、稻痕靈（isoprothiolane)、滅鏽胺 (mepronil)、 氣苯癌咬醇（nuarimol)、 嗟菌靈 (probenazole)、普奎那兹（proquinazid)、比芬諾 (pyrifenox)、百快隆（pyroquilon)、快謹芬（quinoxyfen)、 石夕硫芬（silthiofam)、嗟苯味嗅（thiabendazole)、賽氟滅 (thifluzamide)、甲基·多保淨（thiophanate-methyl)、汰敵寧 (tiadinil)、三賽峻（tricyclazole)、賽福寧（triforine); F.9銅殺真菌劑，諸如紫紅混合物（Bordeaux mixture)、 乙酸銅、鹼性氣氧化銅、鹼式硫酸銅； F.10辅基苯基衍生物，諸如百蜗克（binapacryl)、白粉克 (dinocap)、大脫瞒（dinobuton)、石肖基鄰苯二曱酸異丙基 (nitrophthalisopropyl)； 115703.doc -88 - 200806642 F.11苯°比各，諸如拌種洛（fenpiclonil)或護汰寧 (fludioxonil)； F. 12嗜毯果傘素，諸如亞托敏（azoxystrobin)、地莫菌胺 (dimoxystrobin)、I 氧菌胺（fluoxastrobin)、克收欣 (kresoxim-methyl)、苯氧菌胺（metominostrobin)、奥瑞菌 胺（orysastrobin)、咬氧菌酯（picoxystrobin)或三氟敏 (trifloxystrobin)； F.13次績酸衍生物，諸如四氣丹（captafol)、蓋普丹 (captan)、益發靈（dichlofluanid)、福爾培（folpet)、益洛寧 (tolylfluanid)； F. 14肉桂醯胺類及類似物，諸如達滅芬 (dimethomorph)、敦美醢胺（flumetover)或氟嗎淋 (flumorp)； F. 15硫及其他殺真菌劑，諸如酸化苯并噻二唑-S-甲酯 (acibenzolar-S-methyl)、苯嗟瓦利（benthiavalicarb)、加普 胺（carpropamid)、四氯異苯腈（chlorothalonil)、嗟芬胺 (cyflufenamid)、霜脲氰（cymoxanil)、邁隆（dazomet)、♦璉 菌清（diclomezin)、二氣西莫（diclocymet)、乙黴威 (diethofencarb)、護粒松（edifenphos)、乙 σ塞博胺 (ethaboxam)、環醯菌胺（fenhexamid)、三苯醋錫（fentin-acetate)、禾草靈（fenoxanil)、喊菌腙（ferimzone)、扶吉胺 (fluazinam)、福赛得（fosetyl)、乙填銘（fosetyl-aluminum)、 線黴威（iprovalicarb)、六氯苯（hexachlorobenzene)、美曲 芬諾（metrafenon)、賓克隆（pencycuron)、霜黴威 115703.doc -89- 200806642 (propamocarb)、苯酞（phthalide)、脫克松（t〇lcl〇f〇s_ methyl)、奎脫辛（quintozene)、氯苯醯胺（zoxamide)。 應用 動物害蟲（亦即昆蟲、i知蛛類及線蟲）、植物、植物生長 於其中之土壤或水可藉由此項技術中已知之任一施用方法 與本化合物I或含有其之組合物接觸。如所指，”接觸”包含 直接接觸（將化合物/組合物直接施用於動物害蟲或植物上_ 尤其施用於植物之葉、莖或根）及間接接觸（將化合物/組合 物施用於動物害蟲或植物之所在地）。 式I化合物或包括其之殺蟲組合物可藉由將植物/作物與 殺蟲有效量之式I化合物接觸而用以保護生長中之植物及 作物免受動物害蟲，尤其為昆蟲、粉蟎科或4知蛛類之侵襲 或知染。術§吾&quot;作物π係指生長中及已收獲之作物。 此外’動物害蟲可藉由將目標害愚、其食物供給、棲息 地、滋生地或其所在地與殺蟲有效量之式丨化合物接觸來 控制。如所指，該施用可在藉由害蟲侵染所在地、生長中 之作物或已收穫之作物之前或之後進行。 本發明之化合物亦可預防性地施用於預期會出現害蟲之 地點。 式I化合物亦可藉由將植物與殺蟲有效量之式工化合物接 觸而用以保護生長中之植物免受害蟲之侵襲或侵染。如所 才曰，接觸，包含直接接觸（將化合物/組合物直接施用於害 蟲及/或植物上-尤其施用於植物之葉、莖或根）及間接接觸 (將化合物/組合物施用於害蟲及/或植物之所在地）。 115703.doc -90- 200806642 所在地意謂害蟲或寄生蟲生長或可生長於其中之樓氧 地、滋生地、植物、種子、土壤、區域、材料或環境。 一般而言，”殺蟲有效量”意謂達到對生長之可觀察效應 所需之活性成份之量，所述效應包含壞死、死亡、延遲、 預防及移除、破壞或另外減少目標生物體之出現及活性之 效應。對本發明中所使用之各種化合物/組合物而言，殺 蟲性有效量可變化。殺蟲有效量之組合物亦將根據諸如所 要殺蟲效應及持續時間、天氣、目標物種、所在地、施用 模式及其類似條件之主要條件而變化。 經由接觸(經由土壤、玻璃、牆壁、蚊帳、地毯、植物 部分或動物部分）及攝食（誘餌或植物部分），式以匕合物為 為用於抵抗螞犧、白蟻、黃蜂、蒼 螂，式I化合物較佳用於誘餌組合物中。 誘餌可為液體、固體或半固體製劑(例如凝膠)。 餌可形成為適於各別應用之各種形狀及形式，例如顆粒: =狀、棒狀、盤狀。液體誘_可填充至例如開口容器、+ 務裝置、液滴源或蒸發源之各種裝置中以確保適臂 凝膠可基於水性或油性基質且可經調配以在黏性、：：: 或老化特徵方面滿足特定需要。 ” 用於組合物巾之料為具有足以刺激諸 黃蜂、蒼蠅、蚊子、絲綠雄丄 白犧、 〜蟀荨或蟑螂之昆蟲食取誘餌之 力的產品。吸引*瓦M丄 ^ 丨力了精由使用進食刺激劑或性信息素來# 控。食物刺激劑係 ’、术凋 自（例如）（但不排他地）動物蛋白質及/ 115703.doc •91 - 200806642 或植物蛋白貝（肉粉、魚粉或血粉，昆蟲部分，蛋黃），選 ;自動物源及/或植物源之脂肪及油，或單、寡或多有機釀 類尤其選自蔗糖、乳糖、果糖、右旋糖、葡萄糖、殿 泰、果膠或甚至糖蜜或蜂蜜。果實、作物、植物、動物、 昆蟲之新鮮或腐爛部分或其特定部分亦可用料食刺激 劑。已知性信息素具更強昆蟲特異性。特異性信息素描述 於文獻中且為熟習此項技術者所已知。 作為氣溶膠（例如於喷霧罐中）、油喷霧或泵噴霧之式以匕 合物之調配物高度適於非專業使用者用於控制諸如蒼蠅、 跳蚤n蚊子㈣螂之害蟲。氣溶_錢佳包括活 性混合物，溶劑，諸如低級醇（例如甲醇、乙醇、丙醇、 丁醇），酮（例如丙酮、甲基乙基酮），具有約5〇至25〇。(：之 沸點範圍之石蠟烴（例如煤油），二甲基甲醯胺，n_甲基吡 咯啶酮，二甲亞砜，諸如甲苯、二甲苯之芳族煙，水=此 外諸如乳化劑之助劑，諸如山梨糖醇單油酸酯、具有3_7 mol環氧乙烷之油基乙氧基化物、脂肪醇乙氧基化物，諸 如香精油之芳香油，中級脂肪酸與低級醇形成之酯，芳族 羰基化合物，（若適當）諸如苯曱酸鈉之穩定劑，兩性界面 活性劑，低級環氧化物，原甲酸三乙酯，及（若需要）諸如 丙烷、丁烷、氮、壓縮空氣、二曱基醚、二氧化碳、氧化 亞氮或該等氣體之混合物之推進劑。 油噴霧調配物與氣溶膠配方不同，其不同之處在於油噴 霧調配物中不使用推進劑。 式I化合物及其各別組合物亦可用於蚊香及熏香、煙霧 115703.doc -92- 200806642 筒、汽化器板或長期汽化器中以及防蛀紙、防蛀墊或其它 不依賴熱之汽化器系統中。 用式I化合物及其各別組合物控制藉由昆蟲傳播之傳染 性疾病（例如瘧疾、登革熱及黃熱病、淋巴絲蟲病及利什 曼病（leishmaniasis))之方法亦包括處理棚屋及房屋之表 面、空氣噴霧及浸潰窗簾、帳篷、衣物用品、蚊帳、舌 蠅-捕蠅器或其類似物。應用於纖維、織品、針織品、非 編織品、編網材料或箱及防水布之殺昆蟲性組合物較佳包 括包含殺昆蟲劑、視情況之拒避劑及至少一種黏合劑之混 合物。適合之拒避劑（例如）為队冰二乙基-間甲苯醯胺 (DEET)、N，N-二乙基苯基乙醯胺（DEPA)、^(3·環己+基_ 羰基）-2-甲基哌嗪、（2-羥基甲基環己基）乙酸内酯、2_乙 基-1，3 -己二醇、避蚊酮、甲基新癸醯胺（MNDA)、諸如 {(+/-)-3-烯丙基-2-曱基-4-侧氧基環戊-2-(+)烯基_(+)_反第 一菊酸酯（Esbiothrin)之非用於昆蟲控制之擬除蟲菊酯、得 自如檸檬烯、丁香酚、（+)-優卡醇（Eucamal〇1)(1)、㈠_丨表 優卡酵之植物萃取物或與其一樣，或得自如擰檬桉 (Eucalyptus maculata)、單葉蔓荊（vitex r〇tundifolia)、玫 瑰草（Cymbopogan martinii)、擰檬草（Cymb〇p〇gan citratUS)(擰檬草（lemon grass))、香茅（Cym〇P〇gan nartdus)(香茅（citronella))之植物之粗植物萃取物的拒避 劑。適合之黏合劑係選自（例如）脂族酸之乙烯酯之聚合物 及共聚物（諸如乙酸乙烯酯及維吾爾酸乙烯酯），醇之丙稀 酸酯及曱基丙烯酸酯，諸如丙烯酸丁脂、2-乙基己基丙稀 115703.doc •93- 200806642 :酯：丙烯酸甲醋’諸如苯乙烯之單烯系不飽和烴及二烯 系不飽和烴’及諸如丁二烯之脂族二烯。 浸潰窗簾及蚊帳一般藉由蔣婢 猎由將織物材料浸入殺昆蟲劑之乳 液或W液中或將乳液或分散液喷霧於帳上來進行。 :&quot;物及其組合物可用於保護諸如樹、木柵攔、枕 木权木質材料，及諸如房屋、外屋、工廠之建築物，亦 =建築材料、休具、皮革、纖維、乙烯基物品、電線及電 規等，免遭螞犧及/或白蟣之害，且用於控制螞蟻及/或白 蟻：免危害作物或人類(例如當害蟲侵入房屋及公共設施 中時）。式I化合物不僅施用於周圍土壤表面或地板下土壤 中以保護木質材料，而且其亦可施用於諸如地板下混凝 土、:讀柱、帛、膠合板、傢具等之表面的木材物品，諸 如d H半板等之木製物品及諸如包覆電線、乙稀基薄 片之乙烯基物品，諸如苯乙烯泡沫之絕熱材料等。在抵抗 螞犧危害作物及人類之應用狀況下，本發明之螞犧控制劑 係施用於作物或周圍土壤，或直接施用於螞蟻之巢穴或其 類似物。 在土壤處理或施用於害蟲棲所或巢穴之狀況下，活性成 份之量在每100 m2 〇 〇〇〇1至5〇〇 g，較佳每1〇〇 m2 〇 〇〇1至 2〇 g之範圍内變化。 在材料保護中，習用施用率為（例如）每m2受處理材料 〇·01 §至1000 g活性化合物，理想地為每m2 0.1 g至5〇 g。 用於浸潰材料之殺昆蟲性組合物通常含有〇 〇〇1至95重 量0/。’較佳0.1至45重量％且更佳1至25重量％之至少一種拒 115703.doc •94- 200806642 避劑及/或殺昆蟲劑。 對於用於誘餌組合物而言，活性成份之典型含量為 0.0001重量％至15重量％，理想地為〇 〇〇1重量％至5重量％ 之活性化合物。 對用於噴霧組合物而言，活性成份之含量為0.001至8〇 重量％，較佳〇·〇1至50重量％且最佳〇〇1至15重量％。 對用於處理作物植物而言，本發明之活性成份之施用率 可在每公頃0_1 g至4000 g，理想地每公頃25 §至6〇〇 g，更 理想地每公頃50 g至500 g之範圍内。 種子處理 式I化合物亦適於處理種子以保護種子免遭昆蟲害蟲， 尤其免遭土生昆蟲害蟲且保護所得植物之根及枝免受土壤 害蟲及葉昆蟲。 式I化合物尤其適用於保護種子免遭土壤害蟲且保護所 得植物之根及枝免受土壤害蟲及葉昆蟲。保護所得植物之 根及枝為較佳的。更佳為保護所得植物之枝免遭刺吸式昆 蟲’其t免遭蚜蟲之保護為最佳。 囚此 不㈣包括保護種子免遭昆蟲，尤其免遭土㈣ 蟲且保護苗木之根及枝免遭昆蟲，尤其免遭土壤昆蟲及葉 昆蟲之方法，該方法包括在播種前及/或在發芽後將種子 與通式k化合物或其鹽接觸。尤其較佳者為其中植物之 根及枝受保護之方法，更佳者 1者為其中植物之枝受保護免遭 刺吸式昆蟲之方法，最佳者 光延 勹/、中植物之枝受保護免遭蚜 蟲之方法。 115703.doc -95- 200806642 術語種子涵蓋所有種類之種子及植物繁殖體，其包含 (但不限於）真種子、插條、吸根、球莖、鱗莖、果實、塊 里、殺粒、插枝、伐條及其類似物且在一較佳實施例中咅、 谓真種子。 術扣種子處理包括此項技術中已知之所有適合的種子處 理技術，諸如種子拌藥、種子塗覆、種子撒粉、種子浸= 及種子製丸。 本發明亦包括用活性化合物塗覆或含有活性化合物之種 術語，，塗覆有及/或含有&quot;通常表示視施用方法而定，儘管 或夕或^部分之成份可滲透至繁殖產物中，但在施用時活 性成份大部分位於繁瘦產物之表面上。t (再）種植該繁殖 產物時，其可吸收活性成份。 適合之種子為榖類、根用作物、油料作物、蔬菜、香辛 料、觀賞植物之種子，例如以下各者之種子：硬粒小麥及 其他小麥、大麥、燕麥、黑麥、玉米（飼料玉米及甜玉米/ :及飼料玉米）、黃豆、油料作物、十字花科植物、棉 化、向曰葵、香蕉、水稻、油菜、蒸菁油菜、甜菜、飼料 甜祐子、馬鈴薯、$、草地、草皮、飼料草、番祐、 韭菜、南瓜（pumpkin)/南瓜（SqUash)、甘藍菜、卷心萵苣、 胡椒、黃瓜、瓜、黑芥末（Brassica speeies)、瓜、豆巨碗 =、大蒜、洋蔥、胡蘿葡、諸如馬铃薯之塊莖狀植物、甘 庶、煙草、葡萄、矮牵牛、老鶴草/天竺蔡、三色堇及鳳 仙花。 … 115703.doc -96- 200806642 另外，活性化合物亦可適用於處理來自植物之種子，該 等植物由於包含遺傳工程方法之育種而耐受除草劑或殺真 菌劑或殺昆蟲劑之作用。 舉例而言，活性化合物可用於處理自植物之種子，該等 植物對來自由以下物質組成之群之除草劑有抗性··磺醯 脲、口米嗅琳酮（imidazolinone)、草銨膦（glufosinate-ammonium) 或 草甘膦 異丙銨 （glyphosate-isopropylammonium)及類似活性物質（見（例如译卩-八-0242236、EP_A-242246)(WO 92/00377)(EP-A-0257993、美 國專利第5,013,659號），或用於例如棉花之具有產生使植 物對某些害蟲有抗性之蘇芸金桿菌（Bacillus thuringiensis) 毒素（Bt毒素）的能力之轉殖基因作物植物中（EP-A-0142924、EP-A-0193259) 〇 此外，活性化合物亦可適用於處理來自植物之種子，該 等植物與現存植物相比具有改質特徵，其可（例如）藉由傳 統育種方法及/或產生突變株，或藉由重組程序來產生。 舉例而言，為改質在植物中合成之澱粉（例如WO 92/113 76、WO 92/14827、WO 91/19806)或為具有改質脂 肪酸組合物之轉殖基因作物（WO 91/13972)的目的，已描 述重組改質作物植物之若干事例。 活性化合物之種子處理施用係在植物播種前及植物萌芽 前，藉由對種子喷霧或藉由對種子撒粉來進行。 尤其適用於種子處理之組合物為（例如）： A可溶性濃縮物（SL、LS) 115703.doc •97- 200806642 D 乳液(EW、EO、ES) E 懸浮液（SC、〇D、FS) F水可分散性顆粒及水溶性顆粒（WG、SG) G水可分散性粉末及水溶性粉末（WP、SP、WS) H凝膠調配物（GF) • 1可撒粉之粉末（DP、DS) 習知種子處理調配物包含（例如）可流動性濃縮物FS、溶 液LS、用於乾式處理之粉末ds、用於毁料處理之水可分 散性粉末WS、水溶性粉末SS及乳液ES及EC及凝膠調配物 GF。該等調配物可施用於經稀釋或未經稀釋之種子。對種 子之施用係在播種前直接於種子上進行或在隨後種子發芽 後進行。 在一較佳實施例中，FS調配物係用於種子處理。通常， FS調配物可包括uoo g/1之活性成份、^2〇〇 §/1界面活性 劑、0至200 g/Ι防凍劑、〇至400 g/Ι之黏合劑、〇至2〇〇 g/1 之顏料及高達1公升之溶劑，較佳為水。 用於種子處理之式I化合物之尤其較佳FS調配物通常包 括0.1至80重量％(1至800 gn)之活性成份，0」至20重量％(1 \ 至200 g/Ι)之至少一種界面活性劑，例如〇 〇5至5重量。/〇之 . 濕潤劑及〇·5至15重量％之分散劑，高達20重量％、例如5 至20%之防凍劑，〇至1 5重量％、例如1至15重量％之顏料 及/或染料，0至40重量％、例如1至40重量％之黏合劑（黏附 劑/黏著劑），視情況高達5重量％，例如〇.丨至5%重量之增 稠劑，視情況0·1至2%之消泡劑，及視情況（例如）〇.〇1至1 115703.doc -98- 200806642 重量％之量的諸如殺生物劑、抗氧化劑或其類似物之防腐 劑’及高達100重量％之填充劑/媒劑。 種子處理調配物亦可另外包括黏合劑及視情況著色劑。 可添加黏合劑以改良處理後活性物質在種子上之黏著 力。適合之黏合劑為嵌段共聚物E〇/P〇界面活性劑，且亦 為聚乙烯醇、聚乙烯吡咯啶酮、聚丙烯酸酯、聚甲基丙烯 酸酯、聚丁烯、聚異丁烯、聚苯乙烯、聚乙烯胺、聚乙烯 醯月女、聚乙浠亞胺（Lupas〇i⑧、p〇iymin⑧）、聚鍵、聚胺基 甲酸脂、聚乙酸乙烯酯、甲基纖維素及衍生自該等聚合物 之共聚物。 視情況’著色劑亦可包含於調配物中。用於種子處理調 配物之適合顏料或染料為若丹明（Rh〇(jamin)B、C.I·顏料紅 112、c.i.溶劑紅丨、顏料藍15:4、顏料藍15:3、顏料藍 15:2、顏料藍15:1、顏料藍8〇、顏料黃1、顏料黃13、顏料 紅112、顏料紅48:2 '顏料紅48:1、顏料紅57:1、顏料紅 53:1、顏料燈43、顏料橙34、顏料橙5、顏料綠36、顏料 、、’彔7顏料白6、顏料褐25、驗性紫1 〇、鹼性紫49、酸性紅 5 1、酸性紅52、酸性紅14、酸性藍9、酸性黃23、鹼性紅 1 〇、驗性紅1 〇 8。 •膠凝劑之實例為角叉菜（Satiagel®)。 在種子之處理中，式I化合物之施用率通常為每100 kg種 子0·1 g至10 kg，較佳每100 kg種子1 g至5 kg，更佳每1〇〇 kg種子1 §至1000 g且尤其為每100 kg種子1 g至200 g。對 諸如高苣之特定作物而言，施用率可更高。 115703.doc -99- 200806642 因此，本發明亦係關於包括如本文中所定義之式〗化合 物或I之農業上適用鹽之種子。式Hb合物或其農業上適用 鹽之量一般而言將在每100 kg種子〇1 §至1〇 kg，較佳每 100 kg種子1 g至5 kg，尤其每1〇〇 kg種子1 gj_1000 g範圍 内變化。 動物健康 式I化合物或其對映異構體或其獸醫學上可接受之鹽亦 尤其適於用於對抗動物身體中及動物身體上之寄生蟲。 因此，本發明之一目標亦為提供控制動物身體中及動物 身體上之寄生蟲之新穎方法。本發明之另一目標為提供用 於動物之更安全的殺蟲劑。本發明之另一目標為進一步提 供用於動物之可以比現存殺蟲劑更低之劑量來使用的殺蟲 劑。且本發明之另一目標為提供用於動物之提供寄生蟲之 長期後效控制的殺蟲劑。 本發明亦係關於用於對抗動物身體中及動物身體上之寄 生蟲之組合物，其含有殺寄生蟲有效量之式I化合物或其 對映異構體或其獸醫學上可接受之鹽及可接受之載劑。 本發明亦提供用於處理、控制、預防及保護動物免受寄 生触之钕染及感染之方法，其包括向動物經口、局部或非 左腸扠與或施用殺寄生蟲有效量之式J化合物或其對映異 構體或其獸醫學上可接受之鹽或包括其之組合物。 本I明亦提供製備用於處理、控制、預防或保護動物免 文寄生蟲之侵染及感染之組合物的方法，該組合物包括殺 寄生蟲有效量之式I化合物或其對映異構體或其獸醫學上 115703.doc -100- 200806642 可接受之鹽或包括其之組合物。 化合物抵抗農業害蟲之活性並不暗示其控制動物身體中 及動物身體上之内寄生蟲及外寄生蟲之適合性，其中該等 動物在經口施用之狀況下需要低、非催吐劑量，動物代謝 相容性，低毒性及安全操作。 令人驚訝地，已發現式I化合物適於對抗動物身體中及 動物身體上之内寄生蟲及外寄生蟲。 式I化合物或其對映異構體或其獸醫學上可接受之鹽或 包括其之組合物較佳適用於控制及預防包含溫血動物（包 含人類）及魚之動物的侵染及感染。其（例如）適於控制及預 防以下各者之侵染及感染：哺乳動物，諸如牛、綿羊、 豬、絡騎 ' 鹿、馬、豬、家禽、兔、山羊、犬及描、水 牛、驢、黃鹿及馴鹿；亦及毛皮動物，諸如貂、栗鼠及浣 熊；鳥類，諸如母雞、鵝、火雞及鴨；及魚類，諸如淡水 魚及鹽水魚，諸如鳟魚、鯉魚及鱔魚。 式I化合物或其對映異構體或其獸醫學上可接受之鹽及 包括其之組合物較佳適用於控制及預防諸如犬或貓之家禽 動物之侵染及感染。 溫血動物及魚之侵染包含（但不限於）虱、咬虱、壁虱、 鼻蟲、碑、咬織、薄绳、蒼趨、繩姐病繩幼蟲、恙蟲、 蚋、蚊子及跳蚤。 式I化合物或其對映異構體或其獸醫學上可接受之鹽及 包括其之組合物適於外寄生蟲及/或内寄生蟲之全身性及/ 或非全身性控制。其在所有或—些發育階段中具有抵抗活 115703.doc -101- 200806642 性。 式i化合物尤其適用於對抗外寄生蟲。 式I化合物尤其適用於分別對抗以下各目及物種之寄生 蟲· 跳蚤類（蚤目（Siphonaptera))，例如錨梅頭蚤 (Ctenocephalides felis)、欠觸 f 蛋{Ctenocephalides cards')、 印良良 I (Xenopsylla cheopis)、尺蛋（Pulex irritans)、潛 I (Tunga penetrans)反條故良 KNosopsyllus fasciatus)， 嫜螂類（蜚蠊目（Blattaria-Blattodea))，例如德國小蠊 、亞洲蟑螂aw/zhae)、美 洲大蠊（Perz’p/aweia americana)、日本大蠊（Per(p/aneta japonica) ' ^ ^ {Periplaneta ⑽a)、黑胸大蠊 (Peroplaneta fuligginosa)、激糾繁綠（Periplaneta australasiae) 反東方豐療[Blatta orientalis)， 绳類、蚊類（雙翅目），例如埃及伊蚊（jedes 、白 線伊蚊（deAs 刺擾伊蚊（deda vex⑽s)、墨西 哥橘實繩（d似以ludens)、五斑按蚊（Anopheles maculipennis)、十字按蚊（Anopheles crucians) ^ 白足按蚊 (Anopheles aibimanus)、樣蚊（Anopheies gambiae)、西部癍 蚊（Anopheles freeborni)、白踝癃蚊(Anopheles leucosphyrus)、 槪 4、瘊蚊（Anopheles minimus)、四故癍蚊（Anopheles quadrimaculatus、、紅頭麗祠| WcMa)、姐症金 ^{Chrysomya bezziana) ^ ^ ^i%{Chrysomya hominivorax) ^ 稻金繩、鹿繩、 115703.doc -102- 200806642 鹿斑 it silacea)、大西洋斑 it αί/απ/kz^)、螺旋繩（Coc/z/bmy/a /zomk/vorax)、盾波繩 {Cordylobia anthropophaga)、就侖庫蠓 /wrew)、五帶淡色庫蚊（Cw/ex /7//7/⑼s)、斑蚊（Cw/ex nigripalpus)、％ 帶家故（Culex quinquefasciatus)、媒斑故 {Culex tarsalis、、台 ί%ί 戴故{Culiseta inornata)、票、尾成故 me/awwra)、馬繩/zom/mi)、黃腹廄 繩（77⑽m’a cam’cw/ar/s)、大馬胃繩，&gt;7仏*^/如/以）、 刺舌繩（G70mM(2 、觸舌蠅（G/ow/Na ρα/ρα/ζ、）、 毒舌绳（CJ/ow/wa/wsc/pa)、須舌繩iac/zkoz’As)、 騷擾角绳（T/aemaioWa irritans)、 馬鞍形糠蚊 {Haplodiplosis equestris、、潛緣愚{Hippelates spp·、、反 1 繩lineata) ^ 山谷黑細緣{Leptoconops iorre似）、山羊綠题（Lwcz’/ζ’α caprz’wa)、銅綠繩（Lwez7/a cuprina)、絲光綠绳（LMCz7/a sericata) 、 Lycoria pectoralis、l 黎故屬[Mansonia 、家繩（Mwsca domestica)、鼓藤織（Muscina stabulans) &gt; {Oestrus ov/s)、銀足白蛉（P/z/eftoiomws argeniz’pa)、黑稻田鱗蚊 (Psorophora columbiae)、後色鱗故（Psorophora discolor)、 混合蚋（尸rc&gt;hmw//wm m/xiwm)、紅尾肉繩（Sarcop/zaga /2wmorr/2(9zW(2//*y)、肉绳種（Sarcop/zagflf μ·)、吊蘭蚋 (Simulium vittatum)、i® (Stomoxys calcitrans)、牛 it Z?ovz·⑽*s·)、黑馬虹：⑽s 、細條馬 it (Tabanus lineola)反斑馬 it (Tabanus similis)， 115703.doc -103 - 200806642 風類（藏目（Phthiraptera))，例如人頭為（PW/cw/w humanus capitis)、尺後 KJPediculus humanus corporis)、 ^ {Pthirus pubis) ^ 牛乱、 緒 (Haematopinus suis)、牛韻鼠（Linognathus vituli)、牛 鳥乱ά(9νζ\)、雞乱、大雞風 {Menacanthus stramineus) &gt;5. M si (Solenopotes capillatus) 5 壁風類及寄生瞒類（寄蜗目（Parasitiformes)):壁風類（蜱 亞目（Ixodida))，例如肩月甲真壁風（/xc&gt;(i以scapw/arzi)、全 環硬碑holocyclus)、太平洋硬蜱（/xoda paczyVcws)、棕色犬壁鼠（Rhiphicephalus sanguineus)、安氏 落機山壁風i ⑽(iersom·)、狗矩頭壁乱 {Dermacentor variabilis) 、 美洲 花 蜱(Amblyomma americanum)、墨西哥灣耳爲鼠macw/aiww)、 齧齒壁乱（Orm’i/zoi/orws /zermW)、 回歸熱壁乱 {Ornithodorus iwr/eaia)及寄生蜗類（中氣門亞目 (Mesostigmata))，例如柏氏禽刺蜗（Ornii/zo^yMMs bacoti) 及雞皮刺蜗（De厂仍， 韓蜗亞目（Actinedida)(前氣門亞目（Prostigmata))及粉瞒 亞目（Acaridida)(無氣門亞目（Astigmata))，例如蜂盾蜗屬 (Acarapis spp·)、姬餐編屬（Cheyletiella spp·)、 Ornithocheyletia spp.、良織屬（Myobia spp·、、Psorergates spp·、蹲形蛾屬（Demodex spp·、、·％ 编屬（Trombicula spp·)、犛編屬（Listrophorus spp·)、毛嚢蟲^ 屬（Acarus 115703.doc -104- 200806642 spp,)、食絡編屬（Tyrophagus spp·)、v考本编屬（Caloglyphus spp.) 、 Hypodectes spp· 、 Pterolichus spp·、癢虫茜屬 (Psoroptes spp·)、齋癬 M (Chorioptes spp·)、耳齋癬屬 {Otodectes π/?/?·)、挤蜗屬（ASarcopia 、耳蜗屬 {Notoedres spp.)、Knemidocoptes spp·、Cytodites spp.反反 膜錄 M (Laminosioptes spp)， 椿象類（Heteropterida):溫帶臭蟲/eciw/ar/w)、 熱帶臭蟲（C7mex hemipterus)、老年食蟲椿象（iJMwWws 、錐鼻蟲屬（TV/aioma spp.)、紅腹獵蝽屬 以;?·）、錐墙屬（Pa似ir⑽灯/似 及輪形蟲 critatus) 5Ammonium phthalic acid acetophenone of the formula 及其5 and its preparation have been described in WO 01/70671; WO 02/48137; WO 03/24222 &gt; WO 03/15518, WO 04/67528; WO 04/33468; In /118552. Malononitrile compound CF3(CH2)2C(CN)2CH2(CF2)3CF2H, CF3(CH2)2C (cn)2ch2(cf2)5cf2h, cf3(ch2)2c(cn)2(ch2)2c(cf3)2f, Cf3(ch2)2c(cn)2(ch2)2(cf2)3cf3,cf2h(cf2)3ch2c(cn)2 ch2(cf2)3cf2h,cf3(ch2)2c(cn)2ch2(cf2)3cf3,cf3(cf2 2 ch2c(cn) 2ch2(cf2)3cf2h and cf3cf2ch2c(cn)2ch2(cf2)3 CF2H have been described in WO 05/63694. The fungicidal mixed collateral is one selected from the group consisting of F.1 mercaptoalanines, such as benaxyl, statin 115703.doc -86 - 200806642 (metalaxyl), 吱Ofurace, oxadixyl; F.2 amine derivatives, such as aldimorph, dodine, dodemorph, fenpropimorph, phenyl iron Fenpropidin, guazatine, iminoctadine, spiroxamine, tridemorph; F.3 anilino-based mouth bite, such as pyrimethanil ), mepanipyrim or cyprodinyl; F.4 antibiotics such as cycloheximide, griseofulvin, kasugamycin, natamycin ( Natamycin), polyoxin or streptomycin; F.5. Sitting species, such as bitertanol, bromoconazole, cyproconazole, difenoconazole, dinitroconazole, epoxiconazole, Fenbuconazole, I fluquinconazole, flusilazole, hexaconazole, sputum, J (imazalil), metconazole, micney (McKon) Myclobutanil), penconazole, propiconazole, prochloraz, prothioconazole, tebuconazole, triadimefon, triadimenol, Triflumizole, triticonazole, flutriafol; F.6 dicarboxymethyl imidate, such as iprodion, mecloline 115703.doc -87- 200806642 (myclozolin), procymidon, vinclozolin; F.7 dithiocarbamic acid i, such as ferbate, nabam, mannap (maneb ), manganese powder g (mancozeb), Weibai (metam), free of rotten Metiram), propaneb, polycarbamate, thiram, ziram, zineb; F.8 heterocyclic compounds, such as enemies Anilazine, benomyl, boscalid, carbendazim, carboxin, oxycarboxin, cyazofamid, milong Dazomet), dithianon, dimone, famoxadone, fenamidone, fenarimol, fuberidazole, Flutolanil, furametpyr, isoprothiolane, mepronil, nuarimol, probenazole, proquinazid , pyrifenox, pyroquilon, quinoxyfen, silthiofam, thiabendazole, thifluzamide, methyl·multiple Thiophanate-methyl, tiadinil, tricyclazole, triforin e); F.9 copper fungicide, such as Bordeaux mixture, copper acetate, basic copper oxide, basic copper sulfate; F.10 prophenyl derivative, such as binapacryl , Dinocap, dinobuton, nitrophthalisopropyl; 115703.doc -88 - 200806642 F.11 benzene ratio, such as fenpiclonil or Fludioxonil; F. 12 snails, such as azoxystrobin, dimoxystrobin, fluoxastrobin, kresoxim-methyl, benzene Metominostrobin, oressastrobin, picoxystrobin or trifloxystrobin; F. 13 acid derivatives, such as captafol, cappden (captan), dichlofluanid, folpet, tolylfluanid; F. 14 cinnamylamines and analogues, such as dimethomorph, flumetover or Fluorop; F. 15 sulfur and other fungicides, such as acidified benzothiazide Azibenzolar-S-methyl, benthiavalicarb, carpropamid, chlorothalonil, cyflufenamid, cymoxanil Cymoxanil), dazomet, ♦ diclomezin, diclocymet, diethofencarb, edifenphos, ethaboxam, ringworm Fenhexamid, fentin-acetate, fenoxanil, ferimzone, fluazinam, fosetyl, fosetyl- Aluminum), iprovalicarb, hexachlorobenzene, metrafenon, pencycuron, propamocarb 115703.doc -89-200806642 (propamocarb), phthalide , dextrozine (t〇lcl〇f〇s_ methyl), quintozene, zoxamide. Application of animal pests (i.e., insects, spiders and nematodes), plants, soil or water in which the plants are grown may be contacted with the present compound I or a composition containing the same by any of the application methods known in the art. . As used herein, "contact" includes direct contact (application of the compound/composition directly to animal pests or plants - especially to the leaves, stems or roots of plants) and indirect contact (application of the compound / composition to animal pests or The location of the plant). A compound of formula I or a pesticidal composition comprising the same can be used to protect growing plants and crops from animal pests by contacting the plant/crop with a pesticidally effective amount of a compound of formula I, especially insects, whiteflies Or 4 know the invasion or dyeing of spiders. § I &quot; Crop π refers to growing and harvested crops. In addition, animal pests can be controlled by contacting the target, the food supply, the habitat, the breeding ground or its location with a pesticidally effective amount of the hydrazine compound. As indicated, the application can be carried out before or after the pest infested the location, the growing crop or the harvested crop. The compounds of the invention may also be administered prophylactically to the site where the pest is expected to occur. The compounds of formula I can also be used to protect growing plants from attack or infestation by pests by contacting the plants with a pesticidally effective amount of the formula compound. As used, contact, including direct contact (application of the compound/composition directly to pests and/or plants - especially to the leaves, stems or roots of plants) and indirect contact (application of the compound/composition to pests and / or the location of the plant). 115703.doc -90- 200806642 Location means the growth of a pest or parasite or the growth of a greenhouse, plant, seed, soil, area, material or environment in which it can grow. In general, "insecticidal effective amount" means the amount of active ingredient required to achieve an observable effect on growth, including necrosis, death, delay, prevention and removal, destruction or otherwise reducing the target organism. The effects of appearance and activity. The insecticidal effective amount can vary for the various compounds/compositions used in the present invention. The insecticidally effective amount of the composition will also vary depending on the primary conditions such as the desired insecticidal effect and duration, weather, target species, location, mode of administration, and the like. Through contact (via soil, glass, walls, mosquito nets, carpets, plant parts or animal parts) and feeding (bait or plant parts), the formula is used to resist the sacrifice, termites, wasps, sky, The compound I is preferably used in a bait composition. The bait can be a liquid, solid or semi-solid preparation (e.g., a gel). The bait can be formed into a variety of shapes and forms suitable for the respective application, such as granules: = shape, rod shape, disk shape. The liquid enthalpy can be filled into various devices such as an open container, a cleaning device, a droplet source or an evaporation source to ensure that the arm-like gel can be based on an aqueous or oily matrix and can be formulated to be viscous, ::: or aged The characteristics meet specific needs. The material used for the composition towel is a product that has the power to stimulate the insects of the wasps, flies, mosquitoes, silk green males, white mites, mites or mites. Attracting * watts M 丄 ^ 丨 力The essence is controlled by the use of dietary stimulants or sex pheromones. Food irritants are ', withered (for example) (but not exclusively) animal protein and / 115703.doc •91 - 200806642 or vegetable protein shells (meat, fishmeal) Or blood meal, insect part, egg yolk), selected; automatic source and / or plant source of fat and oil, or single, oligo or organic brewing, especially selected from sucrose, lactose, fructose, dextrose, glucose, Diantai Pectin or even molasses or honey. Fresh or rotted parts of fruits, crops, plants, animals, insects or specific parts thereof may also be used as food stimulants. Known sex pheromones have stronger insect specificity. Specific pheromone description It is known in the literature and is well known to those skilled in the art. As an aerosol (for example in a spray can), an oil spray or a pump spray, the formulation of the composition is highly suitable for non-professional users. Control such as Fly, flea n mosquito (4) pests of cockroaches. Aerosol _ Qian Jia includes active mixture, solvent, such as lower alcohol (such as methanol, ethanol, propanol, butanol), ketone (such as acetone, methyl ethyl ketone), with From about 5 to 25 〇. (: a paraffin hydrocarbon in the boiling range (such as kerosene), dimethylformamide, n-methylpyrrolidone, dimethyl sulfoxide, aromatic smoke such as toluene, xylene, Water = further auxiliary such as emulsifier, such as sorbitol monooleate, oleyl ethoxylate having 3-7 mol of ethylene oxide, fatty alcohol ethoxylate, aromatic oil such as essential oil, intermediate fatty acid An ester formed with a lower alcohol, an aromatic carbonyl compound, if appropriate a stabilizer such as sodium benzoate, an amphoteric surfactant, a lower epoxide, triethyl orthoformate, and, if desired, such as propane or butyl a propellant of a mixture of alkane, nitrogen, compressed air, dimercapto ether, carbon dioxide, nitrous oxide or a mixture of such gases. The oil spray formulation differs from the aerosol formulation in that the oil spray formulation does not use propulsion. Agent The compositions and their individual compositions can also be used in mosquito coils and incense, smoke 115703.doc -92-200806642 cartridges, vaporizer plates or long-term vaporizers as well as anti-mite paper, anti-mite pads or other heat-independent vaporizer systems. The use of compounds of formula I and their individual compositions to control infectious diseases transmitted by insects (such as malaria, dengue and yellow fever, lymphatic filariasis and leishmaniasis) also includes the treatment of sheds and houses Surface, air spray and dipping curtains, tents, clothing items, mosquito nets, tsetse flycatchers or the like. Used in fibers, fabrics, knitwear, non-woven goods, netting materials or boxes and tarps The insecticidal composition preferably comprises a mixture comprising an insecticide, optionally a repellent, and at least one binder. Suitable repellents (for example) are team ice diethyl-m-toluidine (DEET), N,N-diethylphenylacetamide (DEPA), ^(3·cyclohexyl+yl-carbonyl) -2-methylpiperazine, (2-hydroxymethylcyclohexyl)acetic acid lactone, 2-ethyl-1,3-hexanediol, ketoxime, methyl neodecylamine (MNDA), such as { (+/-)-3-allyl-2-mercapto-4-oxocyclopentan-2-(+)alkenyl-(+)-anti-first chrysanthemum (Esbiothrin) Insect-controlled pyrethroids, derived from limonene, eugenol, (+)-eucaol (Eucamal〇1) (1), (a) _ 丨 eucalyptus plant extract or the same, or free Eucalyptus maculata, vitex r〇tundifolia, Cymbopogan martinii, Cymb〇p〇gan citratUS (lemon grass), citronella ( Repellent for crude plant extracts of plants of Cym〇P〇gan nartdus) (citronella). Suitable binders are selected from, for example, polymers and copolymers of vinyl esters of aliphatic acids (such as vinyl acetate and vinyl urate), acrylates of mercaptans and mercapto acrylates, such as butyl acrylate. 2-ethylhexyl propylene 115703.doc •93- 200806642 : ester: methyl acrylate vinegar such as monoethylenically unsaturated hydrocarbons such as styrene and diolefinic unsaturated hydrocarbons and aliphatic dienes such as butadiene . Dipping curtains and mosquito nets are generally carried out by immersing the fabric material in the emulsion or W liquid of the insecticide or spraying the emulsion or dispersion onto the account by Chiang Kai-shek. :&quot;Materials and their compositions can be used to protect wooden materials such as trees, wooden barriers, sleepers, and buildings such as houses, outbuildings, factories, construction materials, rest, leather, fiber, vinyl, Wires and electric gauges are protected from sacrificial and/or chalky and are used to control ants and/or termites: from harm to crops or humans (eg when pests invade houses and public facilities). The compound of formula I is applied not only to the surrounding soil surface or underfloor soil to protect the wood material, but it can also be applied to wood articles such as underfloor concrete, reading columns, crepe, plywood, furniture, etc., such as d H half Wooden articles such as boards and vinyl articles such as covered wires, vinyl-based sheets, heat insulating materials such as styrene foam, and the like. The herbicide control agent of the present invention is applied to a crop or surrounding soil, or directly to an ant's nest or the like, in a state of application against a sacrificial crop and a human. In the case of soil treatment or application to pest habitats or nests, the amount of active ingredient is from 1 to 5 g per 100 m2, preferably from 1 to 2 g per 1 m2. Changes within the scope. In material protection, the conventional application rate is, for example, from m2 to 0.001 to 1000 g of active compound per m2 of treated material, desirably from 0.1 g to 5 g per m2. The insecticidal compositions for impregnating materials typically contain from 1 to 95 weights of 0/. Preferably, at least one of 0.1 to 45% by weight and more preferably 1 to 25% by weight is refractory and/or insecticide. For use in a bait composition, the active ingredient is typically present in an amount from 0.0001% to 15% by weight, desirably from 1% to 5% by weight of the active compound. For use in the spray compositions, the active ingredient is present in an amount of from 0.001 to 8% by weight, preferably from 1 to 50% by weight and most preferably from 1 to 15% by weight. For the treatment of crop plants, the application rate of the active ingredient of the invention may range from 0_1 g to 4000 g per hectare, desirably 25 § to 6 〇〇g per hectare, more desirably 50 g to 500 g per hectare. Within the scope. Seed Treatment The compounds of formula I are also suitable for treating seeds to protect the seeds from insect pests, in particular from indigenous insect pests and to protect the roots and shoots of the resulting plants from soil pests and leaf insects. The compounds of formula I are especially useful for protecting seeds from soil pests and protecting the roots and shoots of the resulting plants from soil pests and leaf insects. It is preferred to protect the roots and branches of the resulting plants. It is more preferable to protect the branches of the obtained plants from the sucking insects, which are best protected from aphids. Prisoners do not (4) include methods to protect seeds from insects, especially from soil (4) insects, and to protect the roots and branches of seedlings from insects, especially soil insects and leaf insects, including before sowing and/or in germination. The seed is then contacted with a compound of formula k or a salt thereof. Particularly preferred is a method in which the roots and branches of the plant are protected, and more preferably one is a method in which the branches of the plant are protected from the sucking insects, and the best ones are protected by light, and the branches of the plants are protected. A method of avoiding mites. 115703.doc -95- 200806642 The term seed covers all kinds of seeds and plant propagules, including but not limited to true seeds, cuttings, roots, bulbs, bulbs, fruits, lumps, granules, cuttings, The strips and their analogs, and in a preferred embodiment, are referred to as true seeds. The seed treatment includes all suitable seed treatment techniques known in the art, such as seed dressing, seed coating, seed dusting, seed dipping, and seed pelleting. The invention also includes the terms of coating or containing the active compound with the active compound, coated and/or contained &quot;generally indicating depending on the method of administration, although the ingredients of the evening or part may penetrate into the reproductive product, However, the active ingredient is mostly on the surface of the lean product when applied. t (re)planting the reproductive product, it absorbs the active ingredient. Suitable seeds are seeds of alfalfa, roots, oil crops, vegetables, spices, ornamental plants, such as seeds of the following: durum wheat and other wheat, barley, oats, rye, corn (feed corn and sweet) Corn / : and feed corn), soybeans, oil crops, cruciferous plants, cotton, hollyhocks, bananas, rice, rapeseed, steamed rapeseed, beets, feed sweets, potatoes, $, grass, turf, feed Grass, Fanyou, Chives, Pumpkin/SqUash, Cabbage, Iceberg Lettuce, Pepper, Cucumber, Melon, Black Mustard (Brassica speeies), Melon, Bean Giant Bowl =, Garlic, Onion, Carrot Portuguese, tuberous plants such as potatoes, kansui, tobacco, grapes, petunia, geranium / scorpion scorpion, pansy and balsam. 115703.doc -96- 200806642 In addition, the active compounds may also be suitable for the treatment of seeds derived from plants which are tolerant to herbicides or fungicides or insecticides due to the breeding of genetic engineering methods. For example, the active compounds can be used to treat seeds from plants which are resistant to herbicides from the group consisting of sulfonylurea, imidazolinone, glufosinate ( Glufosinate-ammonium) or glyphosate-isopropylammonium and similar active substances (see, for example, U.S. Patent No. 8-0242236, EP_A-242246) (WO 92/00377) (EP-A-0257993, US Patent) No. 5,013,659), or for use in transgenic crop plants such as cotton having the ability to produce Bacillus thuringiensis toxin (Bt toxin) which is resistant to certain pests (EP-A- In addition, the active compounds may also be suitable for the treatment of seeds from plants which have a upgrading characteristic compared to existing plants, which can be produced, for example, by conventional breeding methods and/or Mutant strains, or produced by recombinant procedures. For example, starches that are modified for synthesis in plants (eg, WO 92/113 76, WO 92/14827, WO 91/19806) or have modified fatty acid compositions Transgenic gene For the purposes of WO 91/13972, several examples of recombinantly modified crop plants have been described. Seed treatment of active compounds is applied by spraying the seeds or by dusting the seeds before plant sowing and before the plants are germinated. Compositions particularly suitable for seed treatment are, for example: A soluble concentrate (SL, LS) 115703.doc • 97- 200806642 D Emulsion (EW, EO, ES) E suspension (SC, 〇D, FS) F water dispersible granules and water soluble granules (WG, SG) G water dispersible powder and water soluble powder (WP, SP, WS) H gel formulation (GF) • 1 powder that can be dusted ( DP, DS) Conventional seed treatment formulations include, for example, flowable concentrate FS, solution LS, powder ds for dry treatment, water dispersible powder WS for decontamination treatment, water soluble powder SS and Emulsion ES and EC and gel formulation GF. The formulations can be applied to diluted or undiluted seeds. Application to the seed is carried out directly on the seed prior to sowing or after subsequent seed germination. In a preferred embodiment, the FS formulation is for seed treatment. In general, the FS formulation may include uoo g/1 active ingredient, ^2〇〇§1 surfactant, 0 to 200 g/Ι antifreeze, 〇 to 400 g/Ι binder, 〇 to 2〇〇 a pigment of g/1 and a solvent of up to 1 liter, preferably water. Particularly preferred FS formulations of the compound of formula I for seed treatment typically comprise from 0.1 to 80% by weight (1 to 800 gn) of active ingredient, 0 Up to 20% by weight (1 \ to 200 g/Ι) of at least one surfactant, for example 〇〇 5 to 5 by weight. Wetting agent and 〇·5 to 15% by weight of dispersant, up to 20% by weight, for example 5 to 20%, of antifreeze, 〇 to 15% by weight, for example 1 to 15% by weight of pigment and/or Dye, 0 to 40% by weight, for example 1 to 40% by weight of binder (adhesive/adhesive), as the case may be up to 5% by weight, for example 〇. 丨 to 5% by weight of thickener, optionally 0.11 Up to 2% of antifoaming agent, and as appropriate (for example) 至.1 to 1 115703.doc -98- 200806642 by weight of preservatives such as biocides, antioxidants or the like and up to 100 % by weight filler/vehicle. The seed treatment formulation may additionally comprise a binder and optionally a colorant. Adhesives may be added to improve the adhesion of the active substance to the seed after treatment. Suitable binders are block copolymer E〇/P〇 surfactants, and also polyvinyl alcohol, polyvinylpyrrolidone, polyacrylate, polymethacrylate, polybutene, polyisobutylene, polyphenylene. Ethylene, polyvinylamine, polyethylene, female, polyethylenimine (Lupas〇i8, p〇iymin8), poly bonding, polyurethane, polyvinyl acetate, methyl cellulose, and derived therefrom a copolymer of a polymer. Optionally, a colorant may also be included in the formulation. Suitable pigments or dyes for use in seed treatment formulations are rhodamine (jamin B, CI·Pigment Red 112, ci Solvent Red, Pigment Blue 15:4, Pigment Blue 15:3, Pigment Blue 15: 2, pigment blue 15: 1, pigment blue 8 〇, pigment yellow 1, pigment yellow 13, pigment red 112, pigment red 48: 2 'pigment red 48: 1, pigment red 57: 1, pigment red 53: 1, pigment Lamp 43, Pigment Orange 34, Pigment Orange 5, Pigment Green 36, Pigment, '彔7 Pigment White 6, Pigment Brown 25, Vermicular Violet 1 碱性, Basic Violet 49, Acid Red 5 1 , Acid Red 52, Acid Red 14, Acid Blue 9, Acid Yellow 23, Alkaline Red 1 〇, Verification Red 1 〇 8. • An example of a gelling agent is Carrageen (Satiagel®). In the treatment of seeds, the application of the compound of formula I The rate is usually from 0.1 g to 10 kg per 100 kg of seed, preferably from 1 g to 5 kg per 100 kg of seed, more preferably from 1 to 1000 g per 1 kg of seed and especially from 1 g per 100 kg of seed. 200 g. For specific crops such as sorghum, the application rate can be higher. 115703.doc -99- 200806642 Accordingly, the present invention is also directed to an agriculturally applicable salt comprising a compound or I as defined herein. It The amount of the Hb compound or its agriculturally suitable salt will generally be from 1 § to 1 〇 kg per 100 kg of seed, preferably from 1 g to 5 kg per 100 kg of seed, especially per 1 kg of seed. 1 gj_1000 g varies. Animal Health The compound of Formula I or its enantiomer or its veterinary acceptable salt is also particularly suitable for combating parasites in the body of an animal and on the body of an animal. One of the objectives is also to provide a novel method of controlling parasites in the body of an animal and on the body of an animal. Another object of the invention is to provide a safer insecticide for animals. Another object of the invention is to provide further use. An insecticide for use in animals at lower doses than existing insecticides. Another object of the present invention is to provide an insecticide for providing long-term after-effect control of parasites in animals. A composition for combating parasites in the body of an animal and on the body of an animal, comprising a parasiticidally effective amount of a compound of formula I or an enantiomer thereof or a veterinary acceptable salt thereof and an acceptable carrier The invention also mentions A method for treating, controlling, preventing, and protecting an animal from parasitic contact infections and infections, comprising administering to the animal an oral, topical or non-left bowel and or a parasiticidally effective amount of a compound of formula J or Or a veterinary acceptable salt thereof, or a composition comprising the same. The present invention also provides a method of preparing a composition for treating, controlling, preventing or protecting an animal against parasitic infection and infection. The composition comprises a parasiticidally effective amount of a compound of formula I or an enantiomer thereof or a veterinary pharmaceutically acceptable salt thereof, or a composition comprising the same. The resistance of a compound against agricultural pests does not imply its suitability for controlling parasites and ectoparasites in the body of animals and on the body of animals, where such animals require low, non-emetic doses for oral administration, animal metabolism Compatibility, low toxicity and safe handling. Surprisingly, it has been found that the compounds of formula I are suitable for combating parasites and ectoparasites in the body of animals and on the body of animals. The compound of the formula I or its enantiomer or a veterinary acceptable salt thereof or a composition comprising the same is preferably suitable for controlling and preventing infection and infection of animals comprising warm-blooded animals (including humans) and fish. It is, for example, suitable for controlling and preventing infection and infection of mammals such as cattle, sheep, pigs, geese 'deer, horses, pigs, poultry, rabbits, goats, dogs and dogs, buffalo, donkeys , yellow deer and reindeer; also fur animals such as crickets, chinchillas and raccoons; birds such as hens, geese, turkeys and ducks; and fish such as freshwater fish and saltwater fish such as salmon, trout and squid. The compound of the formula I or its enantiomer or a veterinary acceptable salt thereof, and compositions comprising the same, are preferably suitable for controlling and preventing infection and infection of poultry such as dogs or cats. Infection of warm-blooded animals and fish includes (but is not limited to) cockroaches, biting ticks, ticks, larvae, monuments, bite weaves, thin ropes, stagnation, scorpion larvae, mites, crickets, mosquitoes and fleas. . The compound of formula I or its enantiomer or a veterinary acceptable salt thereof, and compositions comprising the same, are suitable for systemic and/or non-systemic control of ectoparasites and/or endoparasites. It has resistance in all or some of the developmental stages 115703.doc -101- 200806642. The compounds of formula i are especially suitable for combating ectoparasites. The compounds of the formula I are especially suitable for the parasites of the following species and species, respectively, for the genus of the genus, the genus of the genus, the genus, the genus, the genus, the genus, the genus, the genus, the genus I (Xenopsylla cheopis), Pulex irritans, Tunga penetrans (Knosopsyllus fasciatus), 嫜螂 (Blattaria-Blattodea), such as German cockroach, Asian 蟑螂aw/ Zhae), Pers'p/aweia americana, Per (p/aneta japonica) ' ^ ^ {Periplaneta (10)a), Peroplaneta fuligginosa, and Periplaneta australasiae ) Blatta orientalis, ropes, mosquitoes (Diptera), such as Aedes aegypti (jedes, Aedes aegypti (deAs harassed Aedes (deda vex (10)s), Mexican orange rope (d seems to Ludens), Anopheles maculipennis, Anopheles crucians ^ Anopheles aibimanus, Anopheies gambiae, Anopheles freeborni, Anophelus Pheles leucosphyrus), 槪4, Anopheles minimus, Anopheles quadrimaculatus, WcMa, and Chrysomya bezziana ^ ^ ^%{Chrysomya hominivorax) ^ Rice Rope, deer rope, 115703.doc -102- 200806642 deer spot it silacea), Atlantic spot it αί/απ/kz^), spiral rope (Coc/z/bmy/a /zomk/vorax), shield wave {Cordylobia Anthropophaga), lunku蠓/wrew), Culex pipiens pallens (Cw/ex /7//7/(9)s), Mosquitoes (Cw/ex nigripalpus),% Culex quinquefasciatus, media {Culex tarsalis, Taiwan % % % { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { , Malaysian stomach rope, &gt;7仏*^/如/以), 刺刺绳 (G70mM (2, contact fly (G/ow/Na ρα/ρα/ζ,), poison tongue rope (CJ/ow/ Wa/wsc/pa), whisker rope iac/zkoz'As), harassment angle rope (T/aemaioWa irritans), saddle-shaped cockroach mosquito {Haplodiplosis equestris, sneak edge {Hippelates spp·, anti-1 rope lineata) ^ Valley Black Fine Edge {Leptoconops ior Relike), Goat Green (Lwcz'/ζ'α caprz'wa), Lungz7/a cuprina, LMCz7/a sericata, Lycoria pectoralis, l Lisman [Mansonia, home rope (Mwsca domestica), Muscina stabulans &gt; {Oestrus ov/s), silver foot white pheasant (P/z/eftoiomws argeniz'pa), black rice field Psorophora columbiae, post-color scale ( Psorophora discolor), mixed sputum (corporate rc > hmw / / wm m / xiwm), red tail meat rope (Sarcop / zaga /2wmorr / 2 (9zW (2 / / * y), meat rope species (Sarcop / zagflf μ ·) , Simulium vittatum, i® (Stomoxys calcitrans), cattle it Z?ovz·(10)*s·), black horse rainbow: (10)s, Tabanus lineola (Tabanus similis), 115703.doc -103 - 200806642 Wind (Phthiraptera), for example, PW/cw/w humanus capitis, KJPediculus humanus corporis), ^ {Pthirus pubis) ^ Haematopinus suis, Linognathus vituli, cows and birds (9νζ\), chicken chaos, big chicken wind {Menacanthus stramineus) &gt;5. M si (Solenopotes cap Illatus) 5 wall winds and parasitic mites (Parasitiformes): wall winds (Ixodida), such as the shoulder wall of the true wall wind (/xc> (i with scapw/arzi), all Ring holocyclus), Pacific hard scorpion (/xoda paczyVcws), brown dog squirrel (Rhiphicephalus sanguineus), Ang's downhill wind i (10) (iersom·), dog head wall chaos {Dermacentor variabilis), American flower A (Amblyomma americanum), Gulf of Mexico ear mouse (macw/aiww), rodent wall chaos (Orm'i/zoi/orws /zermW), returning to the hot wall chaos {Ornithodorus iwr/eaia) and parasitic worms (middle valve suborder) (Mesostigmata)), for example, Ornii/zo^yMMs bacoti and chicken skin thorns (De plant still, Actinedida (Prostigmata) and Aconitidae (Acaridida) (Astigmata), such as Acarapis spp., Cheyletiella spp., Ornithocheyletia spp., Myobia spp., Psorergates spp. Demodex spp·, ·· % Tr (Trombicula spp·), 牦 属 (Listrophorus Spp·), locust genus (Acarus 115703.doc -104-200806642 spp), Tyrophagus spp., vloglyphus spp., Hypodectes spp·, Pterolichus spp· , Psoroptes spp·, Chorioptes spp·, Otodectes π/?/?·, Asarcopia, Notoedres spp., Knemidocoptes spp · Cytodites spp. Laminosioptes spp, Heteropterida: temperate bedbug/eciw/ar/w), tropical bedbug (C7mex hemipterus), old-family insectivore (iJMwWws, Cone genus ( TV/aioma spp.), red-bellied scorpion genus;?·), cone wall genus (Pa-like ir (10) lamp/like and wheel-shaped worm critatus) 5

Anoplurida，例如血風屬吵/?·)、長顎風 屬（Linognathus spp·)、良赵屬（Pediculus spp·)、瘡良屬 {Phtirus spp.、^L 奮 I 爆{Solenopotes spp)，、Anoplurida, for example, bloody winds are noisy/?·), genus (Linognathus spp.), genus Pediculus spp., genus {Phtirus spp., ^L 奋 I blast {Solenopotes spp),

Mallophagida(亞目 Arnblycerina 及 Ischnocerina)，例如 Trimenopon spp.、$% 1 凰{Menopon spp)、鳴 I 凰（Trinoton SPP )、牛見 M (Bovicola spp·)、Werneckiella spp·、 Lepikentron spp·、齧毛鼠屬（Trichodectes spp·)反編羽鼠屬 (Felicola spp.) 5 虫回蟲線蟲綱（Roundworms Nematoda):Mallophagida (Arnblycerina and Ischnocerina), such as Trimenopon spp., $% 1 (Menopon spp), Trinoton SPP, Bovicola spp, Werneckiella spp, Lepikentron spp, Trichodectes spp. Felicola spp. 5 Roundworms Nematoda:

Wipeworm及旋毛蟲類（毛管目（Trichosyringida))，例如 旋毛蟲科（Trichinellidae)「旋毛蟲屬（7&gt;/c/n&gt;e//a spp·))、（鞭 蟲科（Trichuridae))鞭蟲屬（TWc/zwr/s 、毛細線蟲屬 (Capillaria spp)， 115703.doc -105- 200806642 桿形目（Rhabditida)，例如桿絲蟲屬（及spp)、擬 圓蟲屬π/?/?·)、糞類圓線蟲屬 spp)， 圓蟲科（Strongylida)，例如圓蟲屬（iSVrc^a/z^ 57^·)、鉤 義 M (Ancylostoma spp·)、美洲钩義（Necator americanus)、 仰口屬[Bunostomum W·)(鉤蟲）、毛樣線蟲屬 (Trichostrongylus spp·)、撚轉胃蟲 、牛胃絲蟲屬spp.)、庫柏毛樣線蟲 屬[Cooperia spp·、、㈣镇亀（Nematodirus spp·、、鐵 &amp; 象各 屣（Dictyocaulus spp·、、杯 口 象氣屬（Cyathostoma spp·)、綠 節線蟲屬spp·)、賢备（Stephanurus dentatus)、Ollulanus spp·、l % 特屬（Chabertia spp)、賢 義（Stephanurus dentatus) ^ 氣管開嘴蟲（办wgamw trachea)、钩备屬（Ancylostoma spp·)、灣口屬（Uncinaria spp·、、iH 戛（Globocephalus spp·、、板 v 氣氣屬{Necator fPP.)、豬肺蟲屬w·)、毛細苗勒氏肺蟲 {Muellerius capillaris')、琢屬象备屬{Protostrongylus 、住血線蟲屬幻;/ws ·ίφρ.)、擬馬鹿圓屬 {Parelaphostrongylus spp·)、貓肺蟲 abstrusus)反賢象备（Dioctophyma renale)， 腸胃虫回蟲（虫回目（Ascaridida))，例如人虫回蟲 、豬虫回蟲•sz/wm)、雞虫回蟲 galli)、馬虫回蟲（Parascarb equorum)、境备（Enterobius vermicularis)(絲、緣备（Threadworm))、欠细轰（Toxocara 115703.doc -106- 200806642 、獅弓虫回蟲（roxascarb /eom·加）、斯氏尖尾線蟲屬 (Skrjabinema spp·)反馬或氣（Oxyuris equi)， 無唇線蟲目（Camallanida)，例如麥地納龍線蟲 {Dracunculus medinensis){i% ^{guin^di worm)) 5 旋尾目（Spirurida)，例如眼蟲屬（772β/(2ζζ·(3叹户·）、吳策線 義屬（Wuchereria spp,)、布魯格絡轰屬（Brugia spp·)、缚尾 綺、義 M (Onchocerca spp·)、心綺、義屬（Dirofilaria spp·)、雙 瓣綠、氣 M (JDipetalonema spp·)、餐絲、备屬[Setaria spp.)、綠、 紙备屬（Elaeophora sipp.)、血色食道蟲^ (Spirocerca hipi)及 馬胃备屬（Habronema spp·)， 鉤頭蟲類（棘頭蟲目（Acanthocephala))，例如棘頭蟲屬 (Acanthocephalus spp·)、緒 I 頭美（Macracanthorhynchus hirudinaceus)反欠鐵頭氣屬（Oncicola spp)， 满蟲類（扁蟲（Plathelminthes)) ·· 吸蟲類（吸蟲綱（Trematoda))，例如肝吸蟲屬（Facb/a SPP·)、大吸蟲s (Fascioloides magna)、生殖吸备屬 (Paragonimus spp·)、雙脸吸義屬（Dicrocoelium spp·)、年 斯基薑片蟲、中華肝吸蟲（C/onorc/zzi sinensis、、住缸吸義屬（Schistosoma spp·)、毛缸吸義屬 (Trichobilharzia spp·)、有翼 Mr 形吸義（Alaria alata)、生後 吸氣屬（Paragonimus spp·、反 Nanocyetes spp，Wipeworm and Trichinella (Trichosyringida), such as Trichinellidae, Trichinella genus (7&gt;/c/n&gt;e//a spp.), (Trichuridae) whip Genus (TWc/zwr/s, Capillaria spp, 115703.doc -105-200806642 Rhabditida, such as the genus Pythium (and spp), Pseudomonas π/?/? ·), genus Spirulina spp), Strongylida, such as the genus Verticillium (iSVrc^a/z^ 57^·), Angylostoma spp., Necator americanus , genus (Bunostomum W.) (Hookworm), Trichostrong ylus spp., 捻 胃 worm, Bovine genus spp.), Cooperaria genus [Cooperia spp·, (4) Nematodirus spp·, iron &amp; 屣 (Dictyocaulus spp·, Cyathostoma spp·, S. cerevisiae spp·), Stephanurus dentatus, Ollulanus spp·, l % Special (Chabertia spp), Sage (Stephanurus dentatus) ^ Tracheal open mouth (wgamw trachea), Hooked genus (Ancylostoma spp·), Genus (Uncinaria spp·, iH 戛 (Globocephalus spp·, plate v gas genus {Necator fPP.), porcine genus w·), larvae (Muellerius capillaris), genus Subordinates {Protostrongylus, Suspension genus; /ws · ίφρ.), {Parelaphostrongylus spp.), Caterpillar abstrusus, Dioctophyma renale, Gastrointestinal worm (Insect worm) Ascaridida)), such as human worms, worms, sz/wm, gallis, parascarb equorum, Enterobius vermicularis (Threadworm) ), under-fine bombardment (Toxocara 115703.doc -106- 200806642, lion's worm (roxascarb / eom·plus), Skrjabinema spp.) (Oxyuris equi), no lip Camallanida, such as Dracunculus medinensis {i% ^{guin^di worm) 5 Spirurida, such as Euglena (772β/(2ζζ·(3叹户·)) , Wuchereria spp, Brugia spp, bound tail, right M (Onchoc) Erca spp·), heart palpitations, genus Dirofilaria spp., double-lobed green, gas M (JDipetalonema spp.), meal silk, genus [Setaria spp.), green, paper (Elaeophora sipp.), Spirocerca hipi and Habronema spp., Hookworm (Acanthocephala), such as Acanthocephalus spp., I. I. (Macracanthorhynchus) Hirudinaceus) Oncicola spp, Plathelminthes · Trematode (Trematoda), such as Fabb/a SPP·, Fascioloides magna, genus Paragonimus spp., Dicrocoelium spp., C. sinensis, C. sinensis, C/onorc/zzi sinensis, Schistosoma spp., Trichobilharzia spp., Alpha alata, and inhaled genus (Paragonimus spp., anti-Nanocyetes spp,

Cercomeromorpha，尤其為條蟲類（Cestoda)(條蟲），例如 裂頭條 A 屬（DiphyUobothrium spp·)、條義屬（Tenia spp.)、 胞轰屬（Echinococcus spp·)、大條義（Dipylidium caninum)、 115703.doc •107- 200806642 多頭條蟲屬（Mu丨ticeps spp·)、包赎義 M (Hymenolepis SPP·)、申殖孔條备屬（Mesiocestoides spp·)、Vampirolepis SPP·、莫 i良 Mi {Moniezia spp)、裸頭％ 氣 Mi {Anoplocephala SAP·) '迭宮絛蟲π户.）、裸頭絛蟲屬及包膜蟲 屬。 式I化合物及含有其之組合物尤其適用於控制來自雙翅 目、蚤目及蜱亞目之害蟲。 此外，式I化合物及含有其之組合物用於對抗蚊類之用 途尤其較佳。 式I化合物及含有其之組合物用於對抗蠅類之用途為本 發明之另一較佳實施例。 此外，式I化合物及含有其之組合物用於對抗跳蚤類之 用途為尤其較佳的。 式I化合物及含有其之組合物用於對抗壁虱類之用途為 本發明之另一較佳實施例。 式I化合物亦尤其適用於對抗内寄生蟲（蛔蟲線蟲綱、鉤 頭蟲類及渦蟲類）。 投藥可預防性地及治療性地進行。 活性化合物之投藥係直接地進行或以適合之製劑形式經 口，局部/經皮或非經腸進行。 對於向溫血動物經口投藥，式I化合物可調配為動物飼 料、動物飼料預混物、動物飼料濃縮物、丸劑、溶液、糊 狀物、懸浮液、灌服劑、凝膠、錠劑、大丸劑及膠囊。另 外’式I化合物可於動物之飲用水中投與至動物。對於經 115703.doc -108- 200806642 口技樂’所選劑型應向動物提供每天0·01 mg/kg至100 mg/kg動物體重之式〗化合物，較佳為每天〇·5 111§/]^至1〇〇 mg/kg動物體重。 或者，式I化合物可非經腸投與至動物，例如藉由瘤胃 内、肌肉内、靜脈内或皮下注射來投與。式！化合物可分 散或溶於生理上可接受之載劑中用於皮下注射。或者，式 I化合物可調配成植入物用於皮下投藥。另外，式工化合物 可經皮投與至動物。對非經腸投藥而言，所選劑型應每天 向動物提供0.01 mg/kg至100 mg/kg動物體重之式j化合 物。 式I化合物亦可以浸液、微塵、粉末、套環、圓片、喷 霧、洗髮精、點滴及傾倒調配物之形式及以軟膏或水包油 乳液或油包水乳液形式局部地施用於動物。對局部施用而 言，浸液及噴霧通常含有0.5卯111至5,000 ppm且較佳1 ppm 至3,000 ppm之式j化合物。另外，式〗化合物可調配為用於 動物之耳標，尤其為諸如牛及綿羊之四足動物。 適合之製劑為： -溶液，諸如口服溶液、用於稀釋後經口投藥之濃縮物、 用於皮膚上或體腔内之溶液、傾倒調配物、凝膠； 一用於經口投藥或經皮投藥之乳液及懸浮液；半固體製 劑； -活性化合物於軟膏基質中或水包油乳液或油包水乳液基 質中加工之調配物； -固體製劑’諸如粉末、預混物或濃縮物、顆粒、丸劑、 115703.doc -109- 200806642 錠劑、大丸劑、膠囊；氣溶膠及吸入劑，及含活性化合物 之成形物品。 適於注射之組合物係藉由將活性成份溶於適合之溶劑中 且視情況添加去他諸如酸、鹼、缓衝鹽、防腐劑及增溶劑 之成份來製備。將溶液無菌過濾且無菌填充。 適合之溶劑為生理上可耐受之溶劑，諸如水，諸如乙 醇、丁醇、苄醇、甘油、丙二醇、聚乙二醇之烷醇，…甲 基-吼洛啶酮，2-吡咯啶酮，及其混合物。 活性化合物可視情況溶於適於注射之生理上可耐受之植 物油或合成油中。 適合之增溶劑為促進活性化合物溶於主溶劑中或防止其 &gt;儿澱之溶劑。實例為聚乙烯吡咯啶酮、聚乙烯醇、聚氧乙 烯化萬麻油及聚氧乙烯山梨糖醇酯。 適合之防腐劑為苄醇、三氯丁醇、對羥苯甲酸酯及正丁 醇。 口服溶液係直接投與。濃縮物係在稀釋至使用濃度後經 技與口服’谷液及濃縮物係根據當前技術水平及如上文 對注射溶液之描述來製備，無菌程序並非必要的。 用於皮膚上之溶液係滴淋、塗佈、擦拭、噴撒或喷霧於 其上。 用於皮膚上之溶液係根據當前技術水平且 射溶液之描述來製備，無菌程序並非必要的。 其他適合之溶劑為聚丙二醇，苯基乙醇，苯氧基乙醇， 諸如乙酸乙1旨或乙酸m甲㈣自旨之醋，諸如烧二醇 115703.doc -110- 200806642 烧基驗（例如二縮二丙 二 醇單甲醚）之醚，諸如丙酮、甲基 乙基嗣之綱’芳族烴，植物油及合成油，二曱基曱醯 二甲基乙醯胺，二乙二醇單*** (solketal)，碳酸丙二酯，及其混合物。 胺 甘油醇縮丙_ 在製備期間添加增稠劑可為有利的。適合之增稠劑為無 機牦稠诏’諸如膨土、膠狀矽酸、單硬脂酸鋁，有機増稠 片！諸士纖、准素衍生物、聚乙稀醇及其共聚物、丙稀酸醋 及曱基丙稀酸g旨。 疑膝係施用於或塗佈於皮膚上或引人體腔中。凝膠係藉 由用足夠增_處理已如在注射溶液之狀況下所述而製^ 之溶液來製備’該增_為具有軟膏狀稠度效果之透明材 料。所使用之增稠劑為上文所給出之增稠劑。 傾倒調配物係傾倒或喷霧於皮膚之限定區域上，活性化 合物滲透皮膚且起全身性作用。 傾倒调配物係藉由將活性化合物溶解、懸浮或乳化於適 合之皮膚相容性溶劑或溶劑混合物中來製備。若適當，則 添加諸如著色劑、促生物吸收劑、抗氧化劑、光穩定劑、 黏著劑之其他助劑。 適合之溶劑為：水，烷醇’乙二醇’聚乙二醇，聚丙二 醇’甘油’諸如乙醇'苯氧基乙醇之芳醇，諸如 乙酸乙醋、乙酸丁醋、$甲酸节醋之醋，諸如烷二醇烷基 -、、=如一丙—醇單甲醚、二乙二甘醇單丁醚）之醚，諸如 丙酮、甲基乙基酮之酮、諸如碳酸丙二酿、碳酸乙二醋之 環狀碳酸自旨，彡族及/或脂族烴，植物油或合成油， 115703.doc -111- 200806642 DMF，二曱基乙醯胺，諸如曱基吡咯啶酮、正丁基吡咯啶 酮或正辛基吡咯啶酮之正烷基吡咯啶酮，N-甲基吡咯咬 酮，2_吡咯啶酮，2,2-二甲基-4-氧基-亞甲基-1，3_二氧-戊 環及甘油縮甲酸。 適合之著色劑為允許用於動物身體上且可溶解或懸浮之 所有著色劑。 適合之促生物吸收劑為（例如）dmso、諸如十四烷酸異 丙酯、壬酸二丙二醇酯、矽油及其與聚醚之共聚物之塗佈 油，脂肪酸酯，三甘油脂，脂肪醇。 適合之抗氧化劑為亞硫酸鹽或諸如焦亞硫酸鉀之焦亞硫 酸鹽、抗壞血酸、丁基羥基甲笨、丁基羥基大茴香醚、生 育酚。 適合之光穩定劑為（例如）n〇vantis〇lic acid 〇 適合之黏著劑為（例如）纖維素衍生物，澱粉衍生物，聚 丙烯酸酯，諸如褐藻酸酯、明膠之天然聚合物。 乳液可經口、經皮投與或作為注射液來投與。 乳液可為油包水型或為水包油型。 其係精由將活性化合物溶解於疏水相巾或溶解於親水相 中且在適合之乳化劑及(若適當)諸如著色劑、促生物吸收 劑、防腐劑、抗氧化劑、光穩定劑、黏度增強物質之其他 助劑之辅助下，用另—相之溶劑將其均質化而製備。 適合之疏水相（油）為： 植物油，諸如與鏈長Cs_Ci2之植物：二= 115703.doc •112- 200806642 之天然脂肪酸之辛酸/癸酸二甘油酯、三甘油酯混合物的 合成二甘油8旨’亦可能含有羥基之飽和脂肪酸或不飽和脂 肪酸的部分甘油_混合物，c8-c1G脂肪酸之單甘油酯及二 甘油酯，諸如硬脂酸乙酯、己二酸二_正丁醯酯、月桂酸 己醋、二丙二醇壬酸酯之脂肪酸酯，具有中等鏈長之支鏈 脂肪酸與鏈長Ci^Cu之飽和脂肪醇之酯，十四烷酸異丙 酯’棕櫚酸異丙酯，鏈長Cl2_Cl8之飽和脂肪醇之辛酸酯/ 癸酸酯’硬脂酸異丙酯，油醇油酸酯，油酸癸酯，油酸乙 醋’乳酸乙_，諸如合成鴨尾脂腺脂、鄰苯二甲酸二丁 酯、己二酸二異丙酯及與後者相關之酯混合物之蠟狀脂肪 酸酯，諸如異十三烷醇、辛基十二烷醇、十六醇十八醇 (cetylstearyl alcohol)、油醇之脂肪醇，及諸如油酸之脂肪 酸及其混合物。 適合之親水相為：水，諸如丙二醇、乙二醇、山梨糖醇 之醇及其混合物。 適合之乳化劑為： 非離子界面活性劑，例如聚乙氧基化蓖麻油、聚乙氧基 化脫水山梨糖醇單油酸酯、脫水山梨醇單硬脂酸酯、單硬 脂酸甘油酯、單硬脂酸聚氧乙酯、烷基酚聚乙二醇醚； 兩性界面活性劑，諸如N-月桂基-對亞胺基二丙酸二鈉 或卵磷脂； 陰離子界面活性劑，諸如月桂基硫酸鈉、脂肪醇醚硫酸 酯、單/二烷基聚乙二醇醚正磷酸酯單乙醇胺鹽； 1%離子活性界面活性劑’諸如氣化十六烧基三曱基敍。 115703.doc -113 - 200806642 適合之其他助劑為： 缓甲基纖維素、較乳液之物f ’諸如 聚丙烯酸醋、、、^1、、#素及其他纖維素及澱粉衍生物、 t丙佈k S曰、海藻酸明 酮、聚乙烯醇、甲美乙樣其 拉伯膠、聚乙烯°比咯啶 烯基醚與順丁烯二酸酐之共聚物、 '一 、膠狀矽酸或所提及物質之混合物。 =:經口或局部/經皮投與。其係藉由將活性化合 促生物吸收劑、防腐1Γ二 如濕潤劑、著色劑、 來穿備。 W抗氧化劑、光穩定劑之其他助劑 液體懸浮料所有均f溶劑及溶劑混合物。 適t之濕潤劑（分散劑）為上文所給出之乳化劑。 可提及之其他助劑為上文所給出之彼等者。 半固體製劑可經口或局部/經皮投與。其僅由於其較高 之黏度而不同於上文所述之懸浮液及乳液。 4造固體製劑，將活性化合物與適合之賦形劑混合， (若適當）添加助劑且使其達到所要形式。 適口之賦形劑為所有生理上可耐受之固體惰性物質。所 ▲彼等者為無機或有機物質。無機物質為（例如）氣化 =諸如碳_之碳酸鹽、碳酸氫鹽、氧化銘、氧化欽、 ^ ’尼質土、沉澱矽石或膠狀矽石，或磷酸鹽。有機物 、二（彳彳如）糖，纖維素，諸如奶粉、骨粉、榖粉及榖屑之 食物及飼料，澱粉。 I口之助劑為上文已提及之防腐劑、抗氧化劑及/或著 色劑。 115703.doc -114- 200806642 /、他適合之助劑為諸如硬脂酸鎂、硬脂酸、滑石、膨土 之U及動劑’諸如殺粉或交聯聚乙烯^各咬嗣之促 刀解物貝’諸如澱粉、明膠或直鏈聚乙烯吡咯啶酮之黏合 劑，及諸如微晶纖維素之無水黏合劑。 ° 般而s，’’殺寄生蟲有效量”意謂達到對生長之可觀察 效應所需之活性成份之量，所述效應包含壞死、死亡、延 遲、預防及移除、破壞或另外減少目標生物體之出現及活 性之效應°對本發明中所使用之各種化合物/組合物而 吕，殺寄生蟲有效量可變化。殺寄生蟲有效量之組合物亦 將根據諸如所要殺寄生蟲效應及持續時間、目標物種、施 用模式及其類似條件之主要條件而變化。 可用於本發明之組合物通常可包括約〇 〇〇1至％%之式I 化合物。 通否，有利的為以每天0.5 mg/kg至1〇〇 mg/kg，較佳每 天1 mg/kg至50 mg/kg之總量來施用式以匕合物。 即用製劑含有對寄生蟲，較佳為外寄生蟲作用之濃度為 10 ppm至80重量％，較佳為〇1至65重量％，更佳為1至5〇 重量。/。’最佳為5至40重量❹/。之化合物。 在使用前經稀釋之製劑含有對外寄生蟲作用之濃度為 0.5至90重量。/。，較佳為1至5〇重量％之化合物。 此外’製劑包括抵抗内寄生蟲之濃度為丨〇 ρριη至2重量 0/〇 ’較佳為0·05至〇.9重量％，極尤其較佳為〇 〇〇5至〇·25重 量％之式I化合物。 在本發明之一較佳實施例中，包括式以匕合物之組合物 115703.doc •115- 200806642 係經皮/局部施用。 在本發明之另一較佳實施例中，局部施用係以諸如套 ϊ衣、圓片、耳標、固定於身體部分上之帶及黏著條及箔之 含化合物之成形物品形式來進行。 通常，有利的為在3週之過程中，以1〇 mg/kg至3〇〇 mg/kg5：處理動物體重，較佳為2〇 mg/kgs2〇〇 受處 理動物體重，最佳為25 mg/kg至160 mg/kg受處理動物體重 之總量來施用釋放式以匕合物之固體調配物。 為製備成形物品，使用熱塑性及可撓性塑料以及彈性體 及熱塑性彈性體。適合之塑料及彈性體為與式〗化合物足 夠相谷之聚乙烯樹脂、聚胺基曱酸酯、聚丙烯酸酯、環氧 树脂、纖維素、纖維素衍生物、聚醯胺及聚酯。塑料及彈 性體之洋細清單以及成形物品之製備程序係（例如）在w〇 03/086075 中給出。 【實施方式】 本發明現藉由以下實例來進一步詳細說明。 P.製備實例： 實例P_1 · (4-氣-二氫茚_卜基）_(4,5_二氫噻唑_2_基y胺（表i 之化合物實例4 ) 在0C下’向4-氯-二氫茚小基胺（39〇 mg)於二***（2〇 ml)中之溶液中添加1-氯-2-異硫氰基乙烷（283 mg)且在相同 温度下將溶液攪拌2 h。用稀氫氧化鈉溶液中止反應混合 物且用二乙崎萃取。矽膠純化殘餘物以產生240 mg產物 (41%) 〇 115703.doc 200806642 氫-奈-1_基）-(4,5-二氫-嚷嗤-2- 實例 Ρ·2 : (7-氯-1，2,3,4·四 基）-胺（表1之化合物實例9 ) 在〇C下，向7-氣-H3〆-四氫·萘_卜基胺（2〇〇 mg)於二 ***（5 ml)中之溶液中添加卜氯―^異硫氰基乙烷（134 於二乙鱗（5 ml)中之溶液且在相同溫度下將溶液攪拌4 h。 用稀氫氧化鈉溶液中止反應混合物且用二乙_萃取。石夕膠 純化殘餘物以產生171 mg產物（52%)。 C ·式I化合物實例：Cercomeromorpha, especially the Cestoda (Catworm), such as the genus DiphyUobothrium spp., the Tenia spp., the Echinococcus spp., the Dipylidium caninum ), 115703.doc •107- 200806642 (Mu丨ticeps spp·), Hymenolepis SPP·, Mesiocestoides spp·, Vampirolepis SPP·, Mo Yiliang Mi {Moniezia spp), naked head% gas {Anoplocephala SAP·) 'Diangong locust π household.), genus Aphis and Capreolus. The compounds of formula I and compositions containing them are especially useful for controlling pests from the order Diptera, Acarina and Cimicoid. Furthermore, the use of the compounds of the formula I and compositions containing them for combating mosquitoes is especially preferred. The use of the compounds of formula I and compositions containing them for combating flies is another preferred embodiment of the invention. Furthermore, the use of the compounds of the formula I and compositions containing them for combating fleas is especially preferred. The use of the compounds of formula I and compositions containing them for combating ticks is another preferred embodiment of the invention. The compounds of formula I are also particularly suitable for combating endoparasites (aphid nematodes, hookworms and planarians). Administration can be carried out prophylactically and therapeutically. Administration of the active compound is carried out directly or in a suitable formulation, orally, transdermally or parentally. For oral administration to warm-blooded animals, the compound of formula I can be formulated as animal feed, animal feed premix, animal feed concentrate, pill, solution, paste, suspension, dressing, gel, lozenge, Big pills and capsules. Alternatively, the compound of formula I can be administered to an animal in drinking water. For the selected dosage form of 115703.doc -108- 200806642, the animal should be given a compound of 0.01 mg/kg to 100 mg/kg body weight per day, preferably 〇·5 111§/]^ per day. Up to 1 mg/kg animal body weight. Alternatively, the compound of formula I can be administered parenterally to the animal, for example by intratumoral, intramuscular, intravenous or subcutaneous injection. formula! The compound can be dispersed or dissolved in a physiologically acceptable carrier for subcutaneous injection. Alternatively, the compound of formula I can be formulated into an implant for subcutaneous administration. Alternatively, the formula compound can be administered to the animal transdermally. For parenteral administration, the selected dosage form should provide the animal with a compound of formula j from 0.01 mg/kg to 100 mg/kg of body weight per day. The compounds of the formula I can also be applied topically in the form of infusions, dusts, powders, loops, discs, sprays, shampoos, drip and pour-on formulations and in the form of ointments or oil-in-water emulsions or water-in-oil emulsions. animal. For topical application, the infusions and sprays typically contain from 0.5 to 111 to 5,000 ppm and preferably from 1 ppm to 3,000 ppm of the compound of formula j. In addition, the compounds of the formula can be formulated as ear tags for animals, especially tetrapods such as cattle and sheep. Suitable preparations are: - solutions, such as oral solutions, concentrates for oral administration after dilution, solutions for application on the skin or body cavity, pouring formulations, gels; one for oral or transdermal administration Emulsions and suspensions; semi-solid preparations; - formulations of active compounds in ointment bases or in oil-in-water emulsions or water-in-oil emulsion bases; - solid preparations such as powders, premixes or concentrates, granules, Pills, 115703.doc -109- 200806642 Lozenges, boluses, capsules; aerosols and inhalants, and shaped articles containing active compounds. Compositions suitable for injection are prepared by dissolving the active ingredient in a suitable solvent and optionally adding such ingredients such as acid, base, buffer salts, preservatives and solubilizers. The solution was sterile filtered and aseptically filled. Suitable solvents are physiologically tolerated solvents such as water, such as ethanol, butanol, benzyl alcohol, glycerol, propylene glycol, alkanols of polyethylene glycol, methyl-oxazolidinone, 2-pyrrolidone , and mixtures thereof. The active compound may optionally be dissolved in a physiologically tolerable vegetable oil or synthetic oil suitable for injection. Suitable solubilizing agents are those which promote the dissolution of the active compound in the main solvent or prevent it from forming. Examples are polyvinylpyrrolidone, polyvinyl alcohol, polyoxyethyleneated cannabis oil and polyoxyethylene sorbitan ester. Suitable preservatives are benzyl alcohol, trichlorobutanol, parabens and n-butanol. Oral solutions are administered directly. The concentrate is prepared after dilution to the use concentration and the oral &apos; trough and concentrate are prepared according to the state of the art and as described above for the injectable solution. Sterile procedures are not necessary. The solution for application to the skin is dripped, coated, wiped, sprayed or sprayed onto it. Solutions for use on the skin are prepared according to the state of the art and the description of the spray solution, and a sterile procedure is not necessary. Other suitable solvents are polypropylene glycol, phenylethyl alcohol, phenoxyethanol, such as acetic acid ethyl acetate or acetic acid m-(tetra) vinegar, such as glycerol 115703.doc -110-200806642 burning test (for example, deflation) An ether of dipropylene glycol monomethyl ether, such as acetone, methyl ethyl hydrazine, an aromatic hydrocarbon, vegetable oil and synthetic oil, dimercapto dimethyl acetamide, diethylene glycol monoether (solketal), Propylene carbonate, and mixtures thereof. Amine Glycerol Condensation - It may be advantageous to add a thickening agent during preparation. Suitable thickeners are non-organic 牦 诏 such as bentonite, colloidal tannic acid, aluminum monostearate, organic glutinous thick tablets! Zhushi fiber, auxin derivatives, polyethylene glycol and copolymers thereof, acryl vinegar and mercapto acrylate acid. Suspected knees are applied to or applied to the skin or into the body cavity. The gel is prepared by a solution prepared by sufficiently increasing the amount of the solution as described in the case of injecting the solution. The increase is a transparent material having an ointment-like consistency effect. The thickeners used are the thickeners given above. The pour-down formulation is poured or sprayed onto a defined area of the skin, and the active compound penetrates the skin and acts systemically. The pouring formulation is prepared by dissolving, suspending or emulsifying the active compound in a suitable skin compatible solvent or solvent mixture. If appropriate, other auxiliaries such as coloring agents, bioabsorbers, antioxidants, light stabilizers, and adhesives are added. Suitable solvents are: water, alkanol 'ethylene glycol' polyethylene glycol, polypropylene glycol 'glycerol' such as ethanol 'phenoxyethanol aromatic alcohol, such as ethyl acetate, acetic acid butyl vinegar, $ formic acid vinegar, Ethers such as alkanediol alkyl-, = = mono-propanol monomethyl ether, diethylene glycol monobutyl ether, ketones such as acetone, methyl ethyl ketone, such as propylene carbonate, ethylene carbonate Ring-shaped carbonated vinegar, steroid and/or aliphatic hydrocarbon, vegetable oil or synthetic oil, 115703.doc -111- 200806642 DMF, dimethyl acetamide, such as decyl pyrrolidone, n-butyl pyrrolidine N-methylpyrrolidone of ketone or n-octylpyrrolidone, N-methylpyrrolidone, 2-pyrrolidone, 2,2-dimethyl-4-oxy-methylene-1,3 _ Dioxo-pentane and glycerol. Suitable colorants are all colorants which are allowed to be applied to the body of an animal and which are soluble or suspended. Suitable bioabsorbers are, for example, dmso, coating oils such as isopropyl myristate, dipropylene glycol citrate, eucalyptus oil and copolymers thereof with polyethers, fatty acid esters, triglycerides, fats alcohol. Suitable antioxidants are sulfites or pyrosulfites such as potassium metabisulfite, ascorbic acid, butylhydroxymethyl, butylhydroxyanisole, and tocopherol. Suitable light stabilizers are, for example, n〇vantis〇lic acid 〇 Suitable adhesives are, for example, cellulose derivatives, starch derivatives, polyacrylates, natural polymers such as alginates, gelatin. The emulsion can be administered orally, transdermally or as an injection. The emulsion can be water-in-oil or oil-in-water. It is prepared by dissolving the active compound in a hydrophobic phase towel or dissolving in a hydrophilic phase and, in a suitable emulsifier and, if appropriate, such as a coloring agent, a bioabsorber, a preservative, an antioxidant, a light stabilizer, and an enhanced viscosity. Prepared by homogenizing the solvent with another phase with the aid of other auxiliaries of the substance. Suitable hydrophobic phases (oils) are: vegetable oils, such as plants with chain length Cs_Ci2: II = 115703.doc • 112-200806642 The synthesis of diglycerin from the mixture of caprylic/capric acid diglyceride and triglyceride of natural fatty acids 'Alternatively, it may contain a saturated fatty acid of a hydroxyl group or a partial glycerin mixture of an unsaturated fatty acid, a monoglyceride and a diglyceride of a c8-c1G fatty acid, such as ethyl stearate, di-n-butyl decyl adipate, lauric acid. Fatty acid ester of hexanoic acid, dipropylene glycol phthalate, ester of a medium chain length branched chain fatty acid with a chain length Ci^Cu saturated fatty alcohol, isopropyl myristate isopropyl palmitate, chain length Cl2_Cl8 saturated fatty alcohol octanoate / phthalate isopropyl stearyl oleate, oleyl oleate, oleic acid oleate, oleic acid vinegar 'lactic acid B _, such as synthetic duck tail fat gland, neighbor a waxy fatty acid ester of dibutyl phthalate, diisopropyl adipate and an ester mixture associated with the latter, such as isotridecyl alcohol, octyldodecanol, cetylstearyl Alcohol), oleyl alcohol, and fatty acids such as oleic acid Mixture. Suitable hydrophilic phases are: water, such as propylene glycol, ethylene glycol, sorbitol alcohols, and mixtures thereof. Suitable emulsifiers are: nonionic surfactants such as polyethoxylated castor oil, polyethoxylated sorbitan monooleate, sorbitan monostearate, glyceryl monostearate , polyoxyethyl monostearate, alkylphenol polyglycol ether; amphoteric surfactants, such as N-lauryl-p-iminodisodium dipropionate or lecithin; anionic surfactants, such as laurel Sodium sulphate, fatty alcohol ether sulfate, mono/dialkyl polyglycol ether orthophosphate monoethanolamine salt; 1% ionic active surfactant 'such as gasified hexadecanoyl tridecyl. 115703.doc -113 - 200806642 Other suitable additives are: slow methyl cellulose, more emulsions f 'such as polyacrylic acid vinegar,, ^1, ## and other cellulose and starch derivatives, t-propyl Cloth k S曰, alginic acid ketone, polyvinyl alcohol, methyl methacrylate-like Labo gum, copolymer of polyethylene pyrrolidinyl ether and maleic anhydride, 'one, colloidal tannic acid or A mixture of the substances mentioned. =: Oral or topical/transdermal administration. It is prepared by combining an active bio-absorbing agent, a preservative, a wetting agent, and a coloring agent. W Antioxidants, other additives for light stabilizers Liquid suspensions are all f solvents and solvent mixtures. Suitable humectants (dispersants) are the emulsifiers given above. Other auxiliaries which may be mentioned are those given above. Semi-solid preparations can be administered orally or topically/transdermally. It differs from the suspensions and emulsions described above only because of its higher viscosity. 4 A solid preparation is prepared by mixing the active compound with a suitable excipient and, if appropriate, adding an adjuvant and bringing it to the desired form. A palatable excipient is all physiologically tolerable solid inert materials. ▲ They are inorganic or organic substances. The inorganic substance is, for example, gasification = carbonate such as carbon, bicarbonate, oxidized sulphur, oxidized phloem, nucleus, precipitated vermiculite or colloidal vermiculite, or phosphate. Organic matter, two (for example) sugar, cellulose, foods and feeds such as milk powder, bone meal, lotus root starch and swarf, starch. The auxiliaries of the I port are the preservatives, antioxidants and/or coloring agents mentioned above. 115703.doc -114- 200806642 /, his suitable additives are such as magnesium stearate, stearic acid, talc, bentonite U and kinetic agents such as powder-killing or cross-linked polyethylene A binder such as starch, gelatin or linear polyvinylpyrrolidone, and an anhydrous binder such as microcrystalline cellulose. ° s, ''parasite effective amount' means the amount of active ingredient required to achieve an observable effect on growth, including necrosis, death, delay, prevention and removal, destruction or otherwise reducing the target Effect of the appearance and activity of the organism. The effective amount of the parasiticidal agent can vary depending on the various compounds/compositions used in the present invention. The parasiticidally effective amount of the composition will also be sustained according to, for example, the desired parasitic effect. The time, the species of interest, the mode of administration, and the like are varied. The compositions useful in the present invention may generally comprise from about 1% to about 9% of the compound of formula I. By all, advantageously 0.5 mg per day /kg to 1 mg / kg, preferably a total amount of 1 mg / kg to 50 mg / kg per day to apply the formula to the composition. The ready-to-use preparation contains a concentration of parasites, preferably ectoparasites It is from 10 ppm to 80% by weight, preferably from 1 to 65% by weight, more preferably from 1 to 5% by weight, based on the compound of 5 to 40% by weight. Concentration of external parasites from 0.5 to 9 0% by weight, preferably from 1 to 5% by weight of the compound. Further, the formulation comprises a concentration against ectoparasites of 丨〇ρριη to 2% by weight/〇', preferably from 0.05 to 〇.9 by weight. %, very particularly preferably from 5 to 25% by weight of a compound of formula I. In a preferred embodiment of the invention, a composition comprising a compound of the formula 115703.doc • 115- 200806642 Percutaneous/topical application. In another preferred embodiment of the invention, the topical application is formed by a compound such as a tunic, a wafer, an ear tag, a tape attached to a body part, and an adhesive strip and a foil-containing compound. The article form is carried out. Generally, it is advantageous to treat the animal body weight, preferably 2 〇 mg/kg s 2 〇〇 of the treated animal body weight, from 1 〇 mg/kg to 3 〇〇 mg/kg 5 during the course of 3 weeks. The release formulation is a solid formulation of the composition of the treated body, preferably from 25 mg/kg to 160 mg/kg of the body weight of the treated animal. For the preparation of shaped articles, thermoplastic and flexible plastics, as well as elastomers and thermoplastic elastomers are used. Suitable plastics and elastomers are sufficient for the compound of formula Resins, polyamino phthalates, polyacrylates, epoxies, celluloses, cellulose derivatives, polyamines and polyesters, fine lists of plastics and elastomers, and preparation procedures for shaped articles (for example) It is given in WO 03/086075. [Embodiment] The present invention will now be further described in detail by the following examples: P. Preparation Example: Example P_1 · (4-Gas-dihydroindole-bu)_(4, 5_Dihydrothiazole-2-yl yamine (Compound 4 of Table i) A solution of 4-chloro-dihydrofurfurylamine (39 〇mg) in diethyl ether (2 〇ml) at 0C 1-Chloro-2-isothiocyanoethane (283 mg) was added and the solution was stirred at the same temperature for 2 h. The reaction mixture was quenched with dilute sodium hydroxide solution and extracted with diacetyl. The residue was purified by silica gel to give 240 mg of product (41%) 〇115703.doc 200806642 hydrogen-na-1-yl)-(4,5-dihydro-indole-2-example Ρ·2: (7-chloro- 1,2,3,4·tetrayl)-amine (Compound 9 of Table 1) Under 〇C, to 7-gas-H3〆-tetrahydronaphthyl-p-ylamine (2〇〇mg) A solution of chloro-(isothiocyanatoethane) (134 in di-butyl scale (5 ml) was added to the solution in diethyl ether (5 ml) and the solution was stirred at the same temperature for 4 h. The reaction mixture was quenched and extracted with diethyl ether. The residue was purified to afford 171 mg of product (52%).

表1 : 實 例 η R1 [Rim X 物理化學 數據 (熔點[°c]) A B C D 1 1 Η Cl s 163-164 2 1 Η F s 146-147 3 1 Η Br s 168-169 4 1 Η Cl s 171-175 5 1 Η Cl Cl s 137-139 6 1 Η F F s 136-139 7 2 Η Cl Cl s 160-162 8 2 Η Br 161-163 9 2 Η Cl s 168-171 10 1 Η ch3 s 122-127 11 2 Η Br s 174-179 12 1 Η och3 s 143-145 115703.doc •117· 200806642 實 例 η R1 X 物理化學^ 數據 (熔點[°c]) A Β c D 13 1 Η F s 137-141 14 1 Η ~~— och3 ------^ s 126-128 15 1 Η ch3 s 180-182 16 1 Η CN s 121-124 17 1 Η co2ch3 s 204-206 18 1 Η CN s 175-180 19 1 Η Cl s 128-130 ^ 20 1 Η ch3 ch3 s 130-136 21 1 Η CH, ch3 s 165-169 22 1 Η _CH3_ ch3 s 166-168 ' 23 1 Η~ co2ch, s 185-191 — 24 1 Η F s 137-138 ~ 25 1 Η sch3 s 144-146 26 1 Η Cl och3 s 175-177 ^ 27 1 Η CN s 172-175 ^ B ·抵抗害蟲之作用之實例 式I化合物抵抗害蟲之作用係藉由以下實驗來證實： Β· 1 棉虫牙（Cotton Aphid)(棉財（却/ni 藉由將受侵染之葉部分置放於測試植物之頂部，用約 100隻實驗室飼養蚜蟲侵染處於子葉階段之棉植物（品種 ’Delta Pine’）。在24 hr後移除葉部分。將完整植物之子葉 浸入測試化合物之梯度溶液中。5天後，測定相對於對照 植物上之死亡率，在經處理之植物上之蚜蟲死亡率。 在該測試中，與未處理對照相比，300 ppm之化合物實 例第1-6號、第9號、第12號、第13號、第15號、第21號及 第24號展示超過80%之死亡率。 B.2綠桃财（桃虫牙） 藉由將文侵染之葉部分置放於測試植物之頂部，用約4〇 115703.doc -118- 200806642 隻實驗室飼養蚜蟲侵染處於第2葉對階段之胡椒植物（品種 ’California Wonder，）。在24 hr後移除葉部分。將完整植物 之葉浸入測試化合物之梯度溶液中。5天後，測定相對於 對照植物上之死亡率，在經處理之植物上之财蟲死亡率。 在該測試中，與未處理對照相比，3〇〇 ppm之化合物實 例第1-6號、第9號、第號、第12號、第13號、第15號、 第20號、第21號及第24號展示超過80%之死亡率。 115703.doc -119-Table 1: Example η R1 [Rim X Physicochemical data (melting point [°c]) ABCD 1 1 Η Cl s 163-164 2 1 Η F s 146-147 3 1 Η Br s 168-169 4 1 Η Cl s 171 -175 5 1 Η Cl Cl s 137-139 6 1 Η FF s 136-139 7 2 Η Cl Cl s 160-162 8 2 Η Br 161-163 9 2 Η Cl s 168-171 10 1 Η ch3 s 122- 127 11 2 Η Br s 174-179 12 1 Η och3 s 143-145 115703.doc •117· 200806642 Example η R1 X Physicochemical ^ Data (melting point [°c]) A Β c D 13 1 Η F s 137- 141 14 1 Η ~~— och3 ------^ s 126-128 15 1 Η ch3 s 180-182 16 1 Η CN s 121-124 17 1 Η co2ch3 s 204-206 18 1 Η CN s 175- 180 19 1 Η Cl s 128-130 ^ 20 1 Η ch3 ch3 s 130-136 21 1 Η CH, ch3 s 165-169 22 1 Η _CH3_ ch3 s 166-168 ' 23 1 Η~ co2ch, s 185-191 — 24 1 Η F s 137-138 ~ 25 1 Η sch3 s 144-146 26 1 Η Cl och3 s 175-177 ^ 27 1 Η CN s 172-175 ^ B · Examples of compounds against the action of pests of formula I against pests The effect is confirmed by the following experiment: Β· 1 Cotton Aphid (cotton money) (but by placing the infected leaf part on top of the test plant, inoculation of a cotton plant in the cotyledon stage with about 100 laboratory aphids (variety' Delta Pine'). The leaf fraction was removed after 24 hr. The cotyledon of the whole plant was immersed in a gradient solution of the test compound. After 5 days, the mortality of the aphid on the treated plant was determined relative to the mortality on the control plant. rate. In this test, 300 ppm of compound examples Nos. 1-6, No. 9, No. 12, No. 13, No. 15, No. 21 and No. 24 showed more than 80% compared to untreated controls. Mortality. B.2 Green Peach (Peach Insect) By placing the infested leaf portion on top of the test plant, infested with a locust in the laboratory with about 4〇115703.doc -118-200806642 Stage pepper plant (variety 'California Wonder,'). The leaf portion was removed after 24 hr. The leaves of the whole plant are immersed in a gradient solution of the test compound. After 5 days, the mortality of the insects on the treated plants was determined relative to the mortality on the control plants. In this test, 3 〇〇 ppm of compound examples 1-6, 9, 9, 12, 13, 15, 20, 21 No. 24 shows more than 80% mortality. 115703.doc -119-

Claims (1)

200806642 十、申請專利範圍： 種式I之互蜒異構性二氫茚基_或四氫萘基_胺基_唑啉 化合物200806642 X. Patent application scope: The isomerism of the formula I is dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound 式I， 其中 n 為1或2 ; m為1、2、3或4，其中當m為大於^夺，基團R2可具有 相同或不同含義； X 為 〇、S、NR3， 其中R3係選自氫、氰基、硝基、甲醯基、c(=〇) R 、G-C6烧基、c2-c6烯基、c2_c6炔基、c3-c8環烧基、c「C6烷氧基、（^-(^炔基胺基、二 (C2_c6炔基）胺基、（Cl_c6烷氧基）亞甲基、Ci_ C6烷基亞磺醯基、Cl_C6烷基硫基或Ci_c6烷基 石黃醯基，其中該等上述基團之脂族基團中之該 等碳原子可帶有1個、2個或3個彼此獨立地選 自由以下基團組成之群之基團的任一組合··鹵 素、氰基、硝基、羥基、巯基、胺基、羧基、 C^c6燒基、（^匕烷氧基、c2-c6烯基氧基、 C2_C6炔基氧基、Cl_C6鹵烷氧基及Cl_c6烷基硫 115703.doc 200806642 基，或C(0)NR3aR3b、（s〇2)NR3aR3b、苯基、苯 基氧基或苄基，後3個所提及基團之每一者可 未經取代或經1至5個彼此獨立地選自由以下基 團組成之群之基團取代：鹵素、Cl_C6烷基、 Ci_C6鹵烧基、CVC6烧基硫基、Ci-C6_烧基硫 基、C「C6烷氧基及（^-(：6鹵烷氧基；且其中 R3a&amp;R3b各自獨立地為氫、Ci_C6烷基、Ci_C6 鹵烧基、C2-C6烯基或c2-C6炔基； R3c係選自氳、CVC6烷基、C2-C6烯基、c2-c6 炔基、c3-c8環烷基、Cl-c6烷基硫基、Cl_ c6烷氧基、（CVC6烷基）胺基、二（(^(：6烷 基）胺基、苯基及可為含有1個、2個、3個 或4個選自〇、s及N之雜原子之單環或雙 環5至10員雜芳環的雜芳基； Rl係選自氫、氰基、硝基、甲醯基、C(=0)Rlc、Ci-C6 烧基、C2-C6浠基、c2-c6块基、〇3-0：8環燒基、Ci-C6烧氧基、（Ci-C6烧氧基）亞甲基、（^-0：6烧基亞石黃 醯基、Ci-C：6烷基硫基或Cl_C6烷基磺醯基，其中該 等上述基團之脂族基團中之該等碳原子可帶有1 個、2個或3個彼此獨立地選自由以下基團組成之群 之基團的任一組合：_素、氰基、硝基、羥基、巯 基、胺基、叛基、CVC6烧基、（^-(：6烧氧基、c2-c6 烯基氧基、C^C；6炔基氧基、C「C6鹵烷氧基及 烧基硫基，或 C(0)NRlaRlb、（s〇2)NRlaRlb、苯基、 115703.doc -2 - 200806642 笨基氧基或苄基，後3個所提及基團之每一者可未 經取代或經1至5個彼此獨立地選自由以下基團組成 之群之基團取代··齒素、Cl-c0烷基、Ci_C6_烷 土 Ci C0燒基硫基、q-C6鹵烧基硫基、烧氧 基及C^C：6鹵烷氧基；且其中 R a&amp;Rib各自獨立地為氫、c广Q烷基、Ci-Q鹵烷 基、c2-c6烯基或c2-c6炔基； R 係選自氫、c!-c6烧基、c2_c6烯基、c2-c6快 基、C3-C^烷基、c!-C6烷基硫基、CrCs烷氧 基、（CVC6烷基）胺基、二（Cl_c6烷基）胺基、苯 基及可為含有1個、2個、3個或4個選自0、S及 N之雜原子之單環或雙環5至1〇員雜芳環的雜芳 基； R2 係選自鹵素、OH、SH、NH2、S03H、COOH、氰 基、疊氮基、硝基、甲醯基、CONH2、CSNH2、 CH=N-OH 、 CH=N-0-(C1-C6) ^ &amp; 、 C(=0)R2c 、 C(=S)R2e、Ci_C6烧基、c2-C6稀基、C2-C6炔基、C3-c8環烧基、CVC6烷氧基、CVC6烷基胺基、二（Cr C6烧基）胺基、Cl-C8烷基硫基、c2-c6烯基、c2-c6 稀基氧基、c2-c6烯基胺基、c2-c6烯基硫基、c2-c6 快基、c2-c6炔基氧基、c2-C6炔基胺基、c2-c6炔基 硫基、CVC6烷基磺醯基、Cl-C6烷基亞颯基 (alkylsulfoxyl)、c2-C6烯基磺醯基、C2-C6炔基磺醯 基、（c「C6烷氧基）羰基、（C2_C6烯基氧基）羰基、 115703.doc 200806642 (C2-C6快基氧基）-幾基、（Ci_C6烧基）魏基氧基、（C^-C6烯基-)羰基-氧基或（C2-C6炔基-)羰基氧基、（cvc6 烯基）羰基-胺基，其中該等上述基團之脂族基團中 之該等破原子可帶有1個、2個或3個彼此獨立地選 自由以下基團組成之群之基團的任一組合：鹵素、 氰基、硝基、羥基、巯基、胺基、羧基、（^(^烷 基、CVC6烷氧基、c2-c6烯基氧基、c2-C6炔基氧 基、CrC6鹵烷氧基及CrCs烷基硫基； C(0)NR2aR2b、（S〇2)NR2aR2b，其中 ^ 、R各自獨立地選自氫、OH、NH2、烧 基、CrQ鹵烷基、C2-C6烯基或c2-c6炔基； R 係選自氫、烧基、C2-C6烯基、c2-C6炔 基、c3-c8環烧基、（^-(^烷氧基、（Ci-C^疼基） 胺基、一（Ci-C6烧基）胺基、肼基、（Ci-C6烷基） 肼基、二（C^-C：6烷基）肼基、苯基及可為含有i 個、2個、3個或4個選自〇、S及N之雜原子之 單環或雙環5至1 〇員雜芳環的雜芳基； 基團Y-Ar或基團γ-Cy，其中 γ為單鍵、氧、硫、氮、Ci-C6^二基或 二基氧基； Ar為苯基、萘基或含有1個、2個、3個或4個選自 ^個氧、2個硫及3個氮原子之雜原子作為環成 員之單環或雙環5至1()員雜芳環，丨中^係未 經取代或可帶有1至5個彼此獨立地選自由以下 115703.doc 200806642 基團組成之群之基團的任一組合··鹵素、氰 基、硝基、羥基、巯基、胺基、羧基、CrQ 烷基、cvc6鹵烷基、（^-(^烷氧基、C2_C6烯基 氧基、CrC6炔基氧基、Cl-c6鹵烷氧基及Ci_c6 炫基硫基； Cy為環烷基，其未經取代或經個彼此 獨立地選自由以下基團組成之群之基團取代： 鹵素、氰基、硝基、羥基、巯基、胺基、羧 基、CVC6烧基、（VC』烷基、Cl_c^氧基、 C2_C0烯基氧基、C2_C0炔基氧基、Ci-Q鹵烷氧 基及c「c6烷基硫基； 且其中鍵結於該等苯環之相鄰碳原子之基團R 2可連 同該等碳原子形成稠合苯環、稠合飽和或部分不飽 和5員、6員或7員碳環或含有H固、2個、3個或4個 選自2個氧、2個硫及3個氮原子之雜原子作為環成 員之稠合5員、6員或7員雜環，且其中該稠合環係 未經取代或可帶有丨個、2個、3個或4個彼此獨立地 選自由以下基團組成之群之基團：鹵素、氰基、硝 基、羥基、巯基、胺基、羧基、Cl_c6烷基、Ci_c6 烷氧基、CVC6烯基氧基、CVC6炔基氧基、Ci_c6鹵 燒氧基及(^-(:6烷基硫基； 或其對映異構體及/或其農業上及/或獸醫學上可接受之 鹽，其限制條件為式1化合物不為2-(4-硫基-第三丁基d — 二氫茚基胺基）_噁唑啉。 115703.doc 200806642 2 士口今青失 、員1之式1之二氫纟p基-或四氫萘基-胺基坐琳化合 物，其中 係選自氫、氰基、C(=0)Rle、Cl-C6烷基、（：2-(：6烯 基、C2-C6炔基、C3-C8環烷基、Cl-C6烷氧基，且 其中 Rlc係選自氫、Cl-C6烷基、cvc6烯基、c2_c6炔基、 C^C8環燒基、（VC6烧氧基、（Cl-C6烷基）胺基、二 (Ci C6烧基）胺基、笨基及可為含有i個、2個、3個 或4個選自〇、s及N之雜原子之單環或雙環5至1〇員 雜芳環的雜芳基。 3.如明求項丨之式j之二氫茚基_或四氫萘基_胺基_唑啉化合 物，其中R1為氫。 4·如叫求項i之式〗之二氫茚基_或四氫萘基_胺基·唑啉化合 物，其中 R2 係選自氰基、疊氮基、 C〇NH2、S03H、COOH、 C2-C6細基、C2-C6快基、 基、（CVC6烷基）胺基 _ 素、OH、SH、NH2、 C(=〇)R2e、Cl-C6烷基、 〇3&lt;8環烷基、Cl-C6烷氧 二（Ci'C6烷基）胺基，其中該 等上述基團《脂族I®中之該等碳原+可帶有i 個、2個或3個彼此獨立地選自由以下基團組成之群 之基團的任一組合：齒素、氰基、硝基、經基、胺 基、缓基、Cl-C6烧基、cvC6烧氧基、c2_c6稀基氧 基、c2-c6炔基氧|、(:心鹵烷氧基且其中 R2c係選自氫、Cl-c6燒基、C2_C6稀基、 115703.doc -6 - 200806642 基、〇3&lt;8環烷基、Cl_Cj氧基、（Ci-C6烷基） 胺基、二（Ci-C6烷基）胺基、苯基及可為含有1 個、2個、3個或4個選自〇、s及n之雜原子之 單環或雙環5至10員雜芳環的雜芳基。 5·如請求項； 只1&lt;式1之二氫茚基-或四氫萘基-胺基-唑啉化合 物，其中 R 係ί 自氫、烷基、C2-C6烯基、c2-c6炔基、 Cl_C6燒氧基或c3-c8環烷基，其中該等基團可未經 取代’部分或全部_化。 /員1之式I之二氫節基-或四氫萘基-胺基-11 坐.琳化合 /、卞m為3且R2在位置A、C及D處係經取代。 7_如明求項1之式1之二氫茚基-或四氫萘基-胺基-唑啉化合 、甲ni為2且R2在位置A及C處係經取代。 8·如巧求項1之式I之二氫茚基-或四氫萘基-胺基-唑啉化合 物’其中m為2且R2在位置c及D處係經取代。 9·如晴求項1之式I之二氫茚基-或四氫萘基-胺基-唑啉化合 物’其中m為1且R2在位置a處係經取代。 1〇·如清求項1之式I之二氫茚基-或四氫萘基-胺基-唑啉化合 物’其中m為1且R2在位置C處係經取代。 U·如請求項1之式I之二氫茚基-胺基-唑啉化合物，其中η為 1 ° 12·如請求項1之式I之四氫萘基-胺基-唑啉化合物，其中η為 1。 13·如請求項1之式I之二氫茚基-或四氫萘基-胺基-唑啉化合 115703.doc 200806642 物，其中m為2或1。 14. 15. 16. 17. 18. 19. 如明求項1之式Ϊ之二氫茚基_或四氫萘基_胺基_唑啉化合 物，其中X為S或〇。 如明求項1之式〗之二氫茚基-或四氫萘基·胺基_唑啉化合 物’其中X為S。 種農業或獸醫學組合物，其包括至少一種如請求項丄 至1 5中任一項之式j之二氫茚基-或四氫萘基-胺基-唑琳 化a物或其對映異構體及/或其至少一種農業上或獸醫學 上適用之鹽，及至少一種惰性液體及/或固體農藝學上可 接叉之載劑及若須要之至少一種界面活性劑。 種如晴求項1至1 5中任一項之式I之二氫茚基-或四氫萘 基-胺基-唾琳化合物或其對映異構體或其農業上或獸醫 學上可接受之鹽用於對抗動物害蟲的用途。 一種對抗動物害蟲之方法，其包括將該等動物害蟲、其 棲息地、滋生地、食物供給、該等動物害蟲正生長或可 生長於其中之植物、種子、土壤、區域、材料或環境， 或待保護免遭動物侵襲或侵染之材料、植物、種子、土 壌、表面或空間與殺蟲有效量之至少一種如請求項i至 1 5中任一項之式I的二氫茚基_或四氫萘基_胺基_唑啉化 合物或其對映異構體或其至少一種農業上或獸醫學上可 接雙之鹽接觸。 一種保護作物免受動物害蟲之侵襲或侵染之方法，其包 括將作物與殺蟲有效量之至少一種如請求項1至15中任 —項之式I的二氫茚基-或四氫萘基-胺基-唑啉化合物或 115703.doc 200806642 其對映異構體或其至少一種農業上可接受之鹽接觸。 20·如請求項18或19之方法，其中該等動物害蟲為昆蟲、蜘 蛛類或線蟲。 21·如請求項18或19之方法，其中該等動物害蟲為如同翅目 (Homoptera)、鱗翅目（Lepidoptera)或鞘翅目（c〇le〇ptera) 之昆蟲或蜱蜗目（Acarina)之4知蛛類。 22.種保遵種子免遭土壌昆蟲及保護苗木之根及枝免遭昆 虫虫之方法，其包括在播種前及/或發芽後，將該等種子與 殺蟲有效量之如請求項1至1 5中任一項之式I的二氫茚基_ 或四氫萘基-胺基-唑啉化合物或如請求項1至15之其對映 異構體及/或其至少一種農業上可接受之鹽接觸。 23·如請求項22之方法，其中該二氫茚基·或四氫萘基_胺基_ 吐淋化合物係以母100 kg種子0.1 g至10 kg之量來施用。 24·如請求項22或23之方法，其中保護該等所得植物之根及 25. 如請求項22至24之方法，其中保護該等所得植物之枝免 遭蚜蟲。 26. —種種子，其包括每1〇〇 kg種子〇1 §至1〇 kg之量的如請 — 求項1至15中任一項之式I之二氫茚基_或四氫萘基_胺基_ 唾啉化合物或其對映異構體及/或其農業上可接受之鹽。 27· —種如請求項1至15中任一項之式I之二氫茚基_或四氫萘 基-胺基-°圭琳化合物或其對映異構體及/或其至少一種獸 醫學上可接受之鹽的用途，其係用於製造用於對抗動物 身體中或動物身體上之寄生蟲之獸醫學藥劑。 115703.doc 200806642 28. 種製傷用於虛 、、处理、控制、預防或保護動物免受寄生蟲 虫丨、或感木之組合物的方法，其中該組合物包括殺寄 ，蟲有：量之如請求項1至15中任-項之式I的二氫節基_ 或四風萘基·胺基化合物或其對映異構體及/或其獸 醫學上可接受之鹽。 115703.doc 10· 200806642 r 七、指定代表圖： (一) 本案指定代表圖為：（無） (二) 本代表圖之元件符號簡單說明： 八、本案若有化學式時，請揭示最能顯示發明特徵的化學式：Formula I, wherein n is 1 or 2; m is 1, 2, 3 or 4, wherein when m is greater than, the group R2 may have the same or different meaning; X is 〇, S, NR3, wherein R3 is selected From hydrogen, cyano, nitro, carbenyl, c(=〇) R , G-C6 alkyl, c2-c6 alkenyl, c2_c6 alkynyl, c3-c8 cycloalkyl, c "C6 alkoxy, (^-(^ alkynylamino, bis(C2_c6 alkynyl)amine, (Cl_c6 alkoxy)methylene, Ci_C6 alkylsulfinyl, Cl_C6 alkylthio or Ci_c6 alkyl ruthenium, wherein The carbon atoms of the aliphatic groups of the above groups may have one, two or three groups independently selected from the group consisting of the following groups: halogen, cyanide Base, nitro, hydroxy, decyl, amine, carboxyl, C^c6 alkyl, (^ alkoxy, c2-c6 alkenyloxy, C2_C6 alkynyloxy, Cl_C6 haloalkoxy and Cl_c6 alkyl Sulfur 115703.doc 200806642 base, or C(0)NR3aR3b, (s〇2)NR3aR3b, phenyl, phenyloxy or benzyl, each of the latter three mentioned groups may be unsubstituted or 1 to 5 groups independently selected from the group consisting of the following groups Group substitution: halogen, Cl_C6 alkyl, Ci_C6 haloalkyl, CVC6 alkylthio, Ci-C6-alkylthio, C"C6 alkoxy and (^-(:6 haloalkoxy; and wherein R3a&amp; R3b is each independently hydrogen, Ci_C6 alkyl, Ci_C6 haloalkyl, C2-C6 alkenyl or c2-C6 alkynyl; R3c is selected from fluorene, CVC6 alkyl, C2-C6 alkenyl, c2-c6 alkynyl , c3-c8 cycloalkyl, Cl-c6 alkylthio, Cl_c6 alkoxy, (CVC6 alkyl)amine, bis(((6)amino), phenyl and may be 1 , 2, 3 or 4 heteroaryl groups of a monocyclic or bicyclic 5 to 10 membered heteroaryl ring selected from the group consisting of a hetero atom of hydrazine, s and N; R1 is selected from the group consisting of hydrogen, cyano, nitro, and Mercapto group, C(=0)Rlc, Ci-C6 alkyl group, C2-C6 fluorenyl group, c2-c6 block group, 〇3-0:8 ring alkyl group, Ci-C6 alkoxy group, (Ci-C6 burnt) Oxy)methylene, (^-0:6 alkyl sulfite, Ci-C: 6 alkylthio or Cl_C6 alkylsulfonyl, wherein the aliphatic group of the above groups The equivalent carbon atom may carry one, two or three groups independently of each other selected from the group consisting of: _, cyano, nitro, hydroxy, Amino group, amine group, thiol group, CVC6 alkyl group, (^-(:6 alkoxy group, c2-c6 alkenyloxy group, C^C; 6 alkynyloxy group, C"C6 haloalkoxy group and alkyl group Thio group, or C(0)NRlaRlb, (s〇2)NRlaRlb, phenyl, 115703.doc -2 - 200806642 stupyloxy or benzyl, each of the latter three groups may be Substituted or substituted by 1 to 5 groups independently selected from the group consisting of: dentate, Cl-c0 alkyl, Ci_C6_alkane Ci C0 alkylthio, q-C6 halogenated a thio group, an alkoxy group, and a C^C:6 haloalkoxy group; and wherein R a &amp;Rib are each independently hydrogen, c-wide Q-alkyl, Ci-Q haloalkyl, c2-c6 alkenyl or c2- C6 alkynyl; R is selected from the group consisting of hydrogen, c!-c6 alkyl, c2_c6 alkenyl, c2-c6 fast radical, C3-C^alkyl, c!-C6 alkylthio, CrCs alkoxy, (CVC6 Alkyl)amino, bis(Cl_c6 alkyl)amine, phenyl and may be monocyclic or bicyclic 5 to 1 containing 1, 2, 3 or 4 heteroatoms selected from 0, S and N a heteroaryl group of a heteroaryl ring; R2 is selected from the group consisting of halogen, OH, SH, NH2, S03H, COOH, cyano, azido, nitro, methylidene, CONH2, CSNH2 CH=N-OH, CH=N-0-(C1-C6) ^ & , C(=0)R2c, C(=S)R2e, Ci_C6 alkyl, c2-C6 dilute, C2-C6 alkynyl , C3-c8 cycloalkyl, CVC6 alkoxy, CVC6 alkylamino, bis(Cr C6 alkyl)amine, Cl-C8 alkylthio, c2-c6 alkenyl, c2-c6 diloxy , c2-c6 alkenylamino, c2-c6 alkenylthio, c2-c6 fast radical, c2-c6 alkynyloxy, c2-C6 alkynylamino, c2-c6 alkynylthio, CVC6 alkyl Sulfonyl, Cl-C6 alkylsulfoxyl, c2-C6 alkenylsulfonyl, C2-C6 alkynylsulfonyl, (c "C6 alkoxy)carbonyl, (C2_C6 alkenyloxy) )carbonyl, 115703.doc 200806642 (C2-C6 fast oxy)-yl, (Ci_C6 alkyl)-Wikioxy, (C^-C6 alkenyl)carbonyl-oxy or (C2-C6 alkynyl) a) a carbonyloxy group, a (cvc6 alkenyl)carbonyl-amine group, wherein the atomic groups in the aliphatic groups of the above groups may have one, two or three independently selected from the following Any combination of groups of groups consisting of: halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, (^(alkyl, CVC6 alkoxy, c2-c6 alkenyloxy, c2-C6 a oxy group, a CrC6 haloalkoxy group and a CrCs alkylthio group; C(0)NR2aR2b, (S〇2)NR2aR2b, wherein each of R and R is independently selected from the group consisting of hydrogen, OH, NH2, alkyl, CrQ halane a group, a C2-C6 alkenyl group or a c2-c6 alkynyl group; R is selected from the group consisting of hydrogen, alkyl, C2-C6 alkenyl, c2-C6 alkynyl, c3-c8 cycloalkyl, (^-(^ alkoxy) (Ci-C^ pain group) Amine group, mono(Ci-C6 alkyl)amino group, mercapto group, (Ci-C6 alkyl) fluorenyl group, di(C^-C:6 alkyl) fluorenyl group, Phenyl group and heteroaryl group which may be a monocyclic or bicyclic 5 to 1 member heteroaryl ring containing i, 2, 3 or 4 hetero atoms selected from the group consisting of hydrazine, S and N; group Y-Ar Or a group γ-Cy, wherein γ is a single bond, oxygen, sulfur, nitrogen, Ci-C6^diyl or diyloxy; Ar is phenyl, naphthyl or contains 1, 2, 3 or 4 a heterocyclic ring selected from the group consisting of oxygen, 2 sulfur and 3 nitrogen atoms as a ring member, a monocyclic or bicyclic 5 to 1 () heteroaryl ring, which is unsubstituted or may have 1 to 5 Any combination of groups independently selected from the group consisting of 115703.doc 200806642 groups, halogen, cyano, nitro, hydroxy, decyl, amine , carboxy, CrQ alkyl, cvc6 haloalkyl, (^-(^ alkoxy, C2_C6 alkenyloxy, CrC6 alkynyloxy, Cl-c6 haloalkoxy and Ci_c6 thiolthio; Cy is a ring An alkyl group which is unsubstituted or substituted with a group independently selected from the group consisting of: halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, CVC6 alkyl, (VC) An alkyl group, a Cl_coxy group, a C2_C0 alkenyloxy group, a C2_C0 alkynyloxy group, a Ci-Q haloalkoxy group, and a c"c6 alkylthio group; and wherein adjacent carbon atoms bonded to the benzene rings The group R 2 may form a fused benzene ring, a fused or partially unsaturated 5 member, a 6-membered or a 7-membered carbocyclic ring or a H-solid, 2, 3 or 4 selected from 2 together with the carbon atoms. a hetero atom of 2, 6 or 7 members of a hetero atom of oxygen, 2 sulfur and 3 nitrogen atoms, and wherein the fused ring system is unsubstituted or may have one or two , 3 or 4 groups independently selected from the group consisting of halogen, cyano, nitro, hydroxy, decyl, amine, carboxyl, Cl_c6 alkyl, Ci_c6 alkoxy, CVC6 alkenyl Oxygen, CV C6 alkynyloxy, Ci_c6 halooxyl and (^-(6 alkylthio; or an enantiomer thereof and/or an agriculturally and/or veterinarily acceptable salt thereof, the limitations thereof) The compound of formula 1 is not 2-(4-thio-tert-butyld-dihydroindenylamino)-oxazoline. 115703.doc 200806642 2 Shikou Jinqing, member 1 of the formula of dihydroanthracene p- or tetrahydronaphthyl-amine-based compound, which is selected from hydrogen, cyano, C (=0) Rle , Cl-C6 alkyl, (: 2-(:6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, Cl-C6 alkoxy, and wherein Rlc is selected from hydrogen, Cl-C6 alkyl , cvc6 alkenyl, c2_c6 alkynyl, C^C8 cycloalkyl, (VC6 alkoxy, (Cl-C6 alkyl) amine, bis(Ci C6 alkyl) amine, stupid and may contain i , 2, 3 or 4 heteroaryl groups of a monocyclic or bicyclic 5 to 1 member heteroaryl ring selected from the hetero atom of hydrazine, s and N. 3. A fluorenyl- or tetrahydronaphthyl-amino-oxazoline compound, wherein R1 is hydrogen. 4. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula i. Wherein R2 is selected from the group consisting of cyano, azide, C〇NH2, S03H, COOH, C2-C6, K2-C6, ketone, (CVC6 alkyl)amine, OH, SH, NH2 C(=〇)R2e, Cl-C6 alkyl, 〇3&lt;8 cycloalkyl, Cl-C6 alkoxydi(Ci'C6 alkyl)amine, wherein the above groups "aliphatic I The carbonogens + in the ® may have any combination of i, 2 or 3 groups independently selected from the group consisting of dentate, cyano, nitro, thiol, Amine group, buffer group, Cl-C6 alkyl group, cvC6 alkoxy group, c2_c6 diloxy group, c2-c6 alkynyl group|, (: cardamoalkoxy group and wherein R2c is selected from hydrogen, Cl-c6 burnt Base, C2_C6 dilute group, 115703.doc -6 - 200806642 base, 〇3 &lt;8 cycloalkyl, Cl_Cj oxy, (Ci-C6 alkyl) amine, bis(Ci-C6 alkyl)amine, phenyl And may be a heteroaryl group containing 1, 2, 3 or 4 monocyclic or bicyclic 5 to 10 membered heteroaryl rings selected from the group consisting of hydrazines, s and n. 5. If requested; only 1&lt; a dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula 1, wherein R is from hydrogen, alkyl, C2-C6 alkenyl, c2-c6 alkynyl, Cl_C6 alkoxy or c3 a -c8 cycloalkyl group, wherein the groups may be unsubstituted or partially or fully-formed. /1 is a dihydrogenated group of formula I or tetrahydronaphthyl-amino-11.卞m is 3 and R2 is substituted at positions A, C and D. 7_Dihydroindenyl- or tetra-formula of formula 1 Naphthyl-amino-oxazoline compound, a ni is 2 and R2 is substituted at positions A and C. 8. The dihydroindenyl- or tetrahydronaphthyl-amino group of formula I is as claimed. -oxazoline compound 'where m is 2 and R2 is substituted at positions c and D. 9. A dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of formula I, wherein m is 1 and R2 is substituted at position a. 1) A dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula I, wherein m is 1 and R2 is substituted at the position C. U. The dihydroindenyl-amino-oxazoline compound of the formula I of claim 1, wherein n is 1 ° 12. The tetrahydronaphthyl-amino-oxazoline compound of the formula I of claim 1 wherein η is 1. 13. The dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of formula I, claim 1, wherein the m is 2 or 1. 14. 15. 16. 17. 18. 19. The dihydroindenyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula 1 wherein X is S or hydrazine. The dihydroindenyl- or tetrahydronaphthylamino-oxazoline compound of the formula 1 wherein X is S. An agricultural or veterinary composition comprising at least one dihydroindenyl- or tetrahydronaphthyl-amino-azole-based a-form of formula j as claimed in any one of claims 1-5 Isomers and/or at least one agriculturally or veterinaryly applicable salt, and at least one inert liquid and/or solid agronomically compatible carrier and, if desired, at least one surfactant. A dihydroindenyl- or tetrahydronaphthyl-amino-salazine compound of the formula I, or an enantiomer thereof, or an agriculturally or veterinaryly acceptable product thereof, according to any one of claims 1 to 15. The salt received is used against animal pests. A method of combating animal pests, comprising the animal pests, their habitat, breeding grounds, food supply, plants, seeds, soil, areas, materials or environments in which the animal pests are growing or can be grown, or At least one of the material, plant, seed, soil, surface or space and insecticidal effective amount to be protected from infestation or infestation by the animal, such as the indanyl group of formula I, as claimed in any one of claims i to 15 The tetrahydronaphthyl-amino-oxazoline compound or its enantiomer or at least one of its agriculturally or veterinaryly pharmaceutically acceptable salts. A method of protecting a crop from attack or infestation by an animal pest, comprising at least one of a crop and an insecticidally effective amount of a dihydroindenyl- or tetrahydronaphthalene of the formula I as claimed in any one of claims 1 to 15. The amino-amino-oxazoline compound or 115703.doc 200806642 is contacted with its enantiomer or at least one agriculturally acceptable salt thereof. The method of claim 18 or 19, wherein the animal pest is an insect, a spider, or a nematode. The method of claim 18 or 19, wherein the animal pests are insects of the order Homoptera, Lepidoptera, or coleoptera (C〇le〇ptera) or Acarina 4 Know the spiders. 22. A method of protecting a seed from soil insects and protecting the roots and branches of the seedling from insects, including, prior to sowing and/or after germination, the seed and the pesticidal effective amount as in claim 1 The indanyl- or tetrahydronaphthyl-amino-oxazoline compound of the formula I, or the enantiomers thereof according to claims 1 to 15, and/or at least one of them agriculturally Accept the salt contact. The method of claim 22, wherein the dihydroindenyl or tetrahydronaphthylamino group is administered in an amount of from 0.1 g to 10 kg of the parent 100 kg of the seed. The method of claim 22 or 23, wherein the roots of the obtained plants are protected and 25. The method of claim 22 to 24, wherein the branches of the obtained plants are protected from aphids. 26. Seeds comprising dihydroindolyl or tetrahydronaphthyl of formula I according to any one of items 1 to 15 per 1 kg of seed 〇1 § to 1 〇kg An amine group - a porphyrin compound or an enantiomer thereof and / or an agriculturally acceptable salt thereof. 27. The dihydroindenyl- or tetrahydronaphthyl-amino--Guillin compound of the formula I, or any of its enantiomers and/or at least one of the animals of any one of claims 1 to 15 The use of a medically acceptable salt for the manufacture of a veterinary agent for combating parasites in the body of an animal or on the body of an animal. 115703.doc 200806642 28. A method of treating a composition for imaginary, treating, controlling, preventing or protecting an animal from parasitic worms, or sensitizing wood, wherein the composition comprises killing, the worm has: The dihydrogenated benzyl or tetrahydronaphthylamino compound of the formula I in any one of claims 1 to 15 or an enantiomer thereof and/or a veterinary acceptable salt thereof. 115703.doc 10· 200806642 r VII. Designation of Representative Representatives: (1) The representative representative of the case is: (none) (2) The symbol of the symbol of the representative figure is simple: 8. If there is a chemical formula in this case, please reveal the best display. Chemical formula of the inventive feature: 115703.doc115703.doc
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